Cancer therapeutic agents targeting hypoxia-inducible factor-1

Current Medicinal Chemistry

Volumn 18, Issue 21, 2011, Pages 3168-3189

  Wang, R ^a   Zhou, S ^a   Li, S ^a  

^a SHANGHAI JIAO TONG UNIVERSITY   (China)

Author keywords

2 methoxyestradiol; Camptothecins; Direct inhibitors; Geldanamycins; HIF 1 inhibitors; Hypoxia; Hypoxia inducible factor 1; Indirect inhibitors; Mechanism; Polyamides; Polyphenols; Rapamycins; SARs; Shikonin derivatives

Indexed keywords

(ARYLOXYACETYLAMINO)BENZOIC ACID ANALOG; 2 METHOXYESTRADIOL ANALOG; 4 [BIS(2 CHLOROETHYL)OXIDOAMINO]PHENYLALANINE; ANTINEOPLASTIC AGENT; APIGENIN; BENZOAZAHETEROCYCLE; BORTEZOMIB; CAMPTOTHECIN; DEGUELIN; ECHINOMYCIN; EPIDITHIODIKETOPIPERAZINE; FLAVOPIRIDOL; GELDANAMYCIN; HYDROXAMIC ACID; HYPOXIA INDUCIBLE FACTOR 1; HYPOXIA INDUCIBLE FACTOR 1 INHIBITOR; KAEMPFEROL; MOSCATILIN; NAPHTHOQUINONE; NAPHTHOQUINONE SPIROKETAL ANALOG; NSC 13502; PLEUROTIN; POLYAMIDE; POLYPHENOL; PX 12; PX 916; QUERCETIN; QUINOL; RAPAMYCIN; SHIKONIN DERIVATIVE; UNCLASSIFIED DRUG; UNINDEXED DRUG;

ANTINEOPLASTIC ACTIVITY; ARTICLE; BINDING AFFINITY; CANCER CHEMOTHERAPY; CANCER INHIBITION; CONCENTRATION RESPONSE; DNA BINDING; DRUG ANALYSIS; DRUG BINDING; DRUG MECHANISM; DRUG TARGETING; GENE MUTATION; GENETIC TRANSCRIPTION; HUMAN; HYPOXIA; NONHUMAN; PROTEIN EXPRESSION; RNA TRANSLATION; SIGNAL TRANSDUCTION; STRUCTURE ACTIVITY RELATION; TRANSACTIVATION; UPREGULATION;

ANIMALS; ANTINEOPLASTIC AGENTS; GENE EXPRESSION REGULATION, NEOPLASTIC; HUMANS; HYPOXIA-INDUCIBLE FACTOR 1; NEOPLASMS;

EID: 79959955993     PISSN: 09298673     EISSN: 1875533X     Source Type: Journal    
DOI: 10.2174/092986711796391606     Document Type: Article

References (187)

1. Gordan, J. D.; Simon, M. C. Hypoxia-inducible factors: central regulators of the tumor phenotype. Curr. Opin. Genet. Dev., 2007, 17(1), 71-77. (Pubitemid 46109295)
2. Hickey, M. M.; Simon, M. C. Regulation of Angiogenesis by Hypoxia and Hypoxia-Inducible Factors. Curr. Top. Dev. Biol., 2006, 76, 217-257. (Pubitemid 44773777)
3. Rankin, E. B.; Giaccia, A. J. The role of hypoxia-inducible factors in tumorigenesis. Cell Death Differ, 2008, 15(4), 4-685.
4. Li, Y.; Ye, D. Cancer therapy by targeting hypoxia-inducible factor-1. Curr. Cancer Drug Targets, 2010, 10(7), 4-796.
5. Semenza, G. L. Targeting HIF-1 for cancer therapy. Nat. Rev. Cancer, 2003, 3(10), 721-732. (Pubitemid 37328811)
6. Giatromanolaki, A.; Sivridis, E.; Simopoulos, C.; Polychronidis, A.; Gatter, K. C.; Harris, A. L.; Koukourakis, M. I. Hypoxia inducible factors 1a and 2a are associated with VEGF expression and angiogenesis in gallbladder carcinomas. J. Surg. Oncol., 2006, 94(3), 242-247. (Pubitemid 44289989)
7. Puppo, M.; Battaglia, F.; Ottaviano, C.; Delfino, S.; Ribatti, D.; Varesio, L.; Bosco, M. C. Topotecan inhibits vascular endothelial growth factor production and angiogenic activity induced by hypoxia in human neuroblastoma by targeting hypoxia-inducible factor-1α and-2α. Mol. Cancer Ther., 2008, 7(7), 1974-1984.
8. Höckel, M.; Vaupel, P. Tumor hypoxia: Definitions and current clinical, biologic, and molecular aspects. J. Natl. Cancer Inst., 2001, 93(4), 266-276. (Pubitemid 32219813)
9. Teicher, B. A. Hypoxia and drug resistance. Cancer Metastasis Rev., 1994, 13(2), 139-168. (Pubitemid 24220002)
10. Semenza, G. L. Defining the role of hypoxia-inducible factor 1 in cancer biology and therapeutics. Oncogene, 2010, 29(5), 4-634.
11. Ravizza, R.; Molteni, R.; Gariboldi, M. B.; Marras, E.; Perletti, G.; Monti, E. Effect of HIF-1 modulation on the response of two-and three-dimensional cultures of human colon cancer cells to 5-fluorouracil. Eur. J. Cancer, 2009, 45(5), 890-898.
12. Sasabe, E.; Zhou, X.; Li, D.; Oku, N.; Yamamoto, T.; Osaki, T. The involvement of hypoxia-inducible factor-1α in the susceptibility to γ-rays and chemotherapeutic drugs of oral squamous cell carcinoma cells. Int. J. Cancer, 2007, 120(2), 4-277.
13. Lee, J. W.; Bae, S. H.; Jeong, J. W.; Kim, S. H.; Kim, K. W. Hypoxiainducible factor (HIF-1)α: Its protein stability and biological functions. Exp. Mol. Med., 2004, 36(1), 4-12.
14. Semenza, G. L. HIF-1 and mechanisms of hypoxia sensing. Curr. Opin. Cell Biol., 2001, 13(2), 167-171. (Pubitemid 32209217)
15. Barginear, M. F.; Van Poznak, C.; Rosen, N.; Modi, S.; Hudis, C. A.; Budman, D. R. The heat shock protein 90 chaperone complex: An evolving therapeutic target. Curr. Cancer Drug Targets, 2008, 8(6), 522-535.
16. Katschinski, D. M.; Le, L.; Schindler, S. G.; Thomas, T.; Voss, A. K.; Wenger, R H. Interaction of the PAS B domain with HSP90 accelerates hypoxia-inducible factor-1α stabilization. Cell. Physiol. Biochem., 2004, 14(4-6), 351-360. (Pubitemid 39179204)
17. Isaacs, J. S.; Jung, Y. J.; Mimnaugh, E. G.; Martinez, A.; Cuttitta, F.; Neckers, L. M. Hsp90 regulates a von Hippel Lindau-independent hypoxiainducible factor-1 alpha-degradative pathway. J. Biol. Chem., 2002, 277(33), 29936-29944.
18. Zhou, J.; Brüne, B. Cytokines and hormones in the regulation of hypoxia inducible factor-1α (HIF-1α). Cardiovasc Hematol Agents Med Chem, 2006, 4(3), 189-197. (Pubitemid 44027709)
19. Ghayad, S. E.; Cohen, P. A. Inhibitors of the PI3K/Akt/mTOR pathway: new hope for breast cancer patients. Recent Pat Anticancer Drug Discov, 2010, 5(1), 29-57.
20. Kaluz, S.; Kaluzová, M.; Stanbridge, E. J. Regulation of gene expression by hypoxia: Integration of the HIF-transduced hypoxic signal at the hypoxiaresponsive element. Clin. Chim. Acta, 2008, 395(1-2), 6-13.
21. Jacobs, C. S.; Dervan, P. B. Modifications at the C-terminus to improve pyrrole-imidazole polyamide activity in cell culture. J. Med. Chem., 2009, 52(23), 7380-7388.
22. Jones, D. T.; Harris, A. L. Identification of novel small-molecule inhibitors of hypoxia-inducible factor-1 transactivation and DNA binding. Mol. Cancer Ther., 2006, 5(9), 2193-2202. (Pubitemid 44530455)
23. Kong, D.; Park, E. J.; Stephen, A. G.; Calvani, M.; Cardellina, J. H.; Monks, A.; Fisher, R J.; Shoemaker, R H.; Melillo, G. Echinomycin, a smallmolecule inhibitor of hypoxia-inducible factor-1 DNA-binding activity. Cancer Res., 2005, 65(19), 9047-9055. (Pubitemid 41377397)
24. Vlaminck, B.; Toffoli, S.; Ghislain, B.; Demazy, C.; Raes, M.; Michiels, C. Dual effect of echinomycin on hypoxia-inducible factor-1 activity under normoxic and hypoxic conditions. FEBS J., 2007, 274(21), 5533-5542. (Pubitemid 47622065)
25. Shin, D. H.; Chun, Y. S.; Lee, D. S.; Huang, L. E.; Park, J. W. Bortezomib inhibits tumor adaptation to hypoxia by stimulating the FIH-mediated repression of hypoxia-inducible factor-1. Blood, 2008, 111(6), 3131-3136.
26. Yeo, E. J.; Ryu, J. H.; Cho, Y. S.; Chun, Y. S.; Huang, L. E.; Kim, M. S.; Park, J. W. Amphotericin B blunts erythropoietin response to hypoxia by reinforcing FIH-mediated repression of HIF-1. Blood, 2006, 107(3), 916-923. (Pubitemid 43156287)
27. Cook, K. M.; Hilton, S. T.; Mecinovic, J.; Motherwell, W. B.; Figg, W. D.; Schofield, C. J. Epidithiodiketopiperazines block the interaction between hypoxia-inducible factor-1α (HIF-1α) and p300 by a zinc ejection mechanism. J. Biol. Chem., 2009, 284(39), 26831-26838.
28. Mukherjee, A.; Huber, K.; Evans, H.; Lakhani, N.; Martin, S. A cellular and molecular investigation of the action of PMX464, a putative thioredoxin inhibitor, in normal and colorectal cancer cell lines. Br. Brr. J. Pharmacol., 2007, 151(8), 1167-1175. (Pubitemid 47255909)
29. Jones, D. T.; Pugh, C. W.; Wigfield, S.; Stevens, M. F. G.; Harris, A. L. Novel thioredoxin inhibitors paradoxically increase hypoxia-inducible factora expression but decrease functional transcriptional activity, DNA binding, and degradation. Clin. Cancer. Res., 2006, 12(18), 5384-5394. (Pubitemid 44497252)
30. Arcamone, F.; Penco, S.; Orezzi, P.; Nicolella, V.; Pirelli, A. Structure and synthesis of distamycin a [15]. Nature, 1964, 203(4949), 4-1065.
31. Zhu, S. L.; Gao, P. H.; Li, P.; Jiang, Y. Y.; Zhang, D. Z. Advances in the chemical and biological studies of polyamides. Yaoxue Xuebao, 2008, 43(11), 1089-1093.
32. Lamamie De Clairac, R. P.; Geierstanger, B. H.; Mrksich, M.; Dervan, P. B.; Wemmer, D. E. NMR characterization of hairpin polyamide complexes with the minor groove of DNA. J. Am. Chem. Soc., 1997, 119(34), 7909-7916. (Pubitemid 27380250)
33. Olenyuk, B. Z.; Zhang, G. J.; Klco, J. M.; Nickols, N. G.; Kaelin Jr., W. G.; Dervan, P. B. Inhibition of vascular endothelial growth factor with a sequence-specific hypoxia response element antagonist. Proc. Natl. Acad. Sci. U. S. A., 2004, 101(48), 16768-16773. (Pubitemid 39601313)
34. Nickols, N. G.; Jacobs, C. S.; Farkas, M. E.; Dervan, P. B. Improved nuclear localization of DNA-binding polyamides. NAR, 2007, 35(2), 363-370. (Pubitemid 46237387)
35. Kageyama, Y.; Sugiyama, H.; Ayame, H.; Iwai, A.; Fujii, Y.; Huang, L. E.; Kizaka-Kondoh, S.; Hiraoka, M.; Kihara, K. Suppression of VEGF transcription in renal cell carcinoma cells by pyrrole-imidazole hairpin polyamides targeting the hypoxia responsive element. Acta Oncol., 2006, 45(3), 317-324. (Pubitemid 43675573)
36. Nickols, N. G.; Jacobs, C. S.; Farkas, M. E.; Dervan, P. B. Modulating hypoxia-inducible transcription by disrupting the HIF-1-DNA interface. ACS Chem. Biol., 2007, 2(8), 4-571.
37. Viger, A.; Dervan, P. B. Exploring the limits of benzimidazole DNA-binding oligomers for the hypoxia inducible factor (HIF) site. Bioorg. Med. Chem., 2006, 14(24), 8539-8549. (Pubitemid 44667530)
38. Bando, T.; Sugiyama, H. Synthesis and biological properties of sequencespecific DNA-alkylating pyrrole-imidazole polyamides. Acc. Chem. Res., 2006, 39(12), 935-944.
39. Pallis, M.; Yoshida, M.; Bradshaw, T.; Westwell, A.; Grundy, M.; Stevens, M.; Russell, N. Expression of thioredoxin in primary AML and induction of apoptosis by the thioredoxin-inhibitory compound AW464. Blood, 2001, 98 (11 PART I).
40. Mukherjee, A.; Westwell, A. D.; Bradshaw, T. D.; Stevens, M. F. G.; Carmichael, J.; Martin, S. G. Cytotoxic and antiangiogenic activity of AW464 (NSC 706704), a novel thioredoxin inhibitor: An in vitro study. Br. J. Cancer., 2005, 92(2), 350-358. (Pubitemid 40343152)
41. Powis, G.; Wipf, P.; Lynch, S. M.; Birmingham, A.; Kirkpatrick, D. L. Molecular pharmacology and antitumor activity of palmarumycin-based inhibitors of thioredoxin reductase. Mol. Cancer Ther., 2006, 5(3), 630-636.
42. Welsh, S. J.; Williams, R R.; Birmingham, A.; Newman, D. J.; Kirkpatrick, D. L.; Powis, G. The thioredoxin redox inhibitors 1-methylpropyl 2-imidazolyl disulfide and pleurotin inhibit hypoxia-induced factor 1alpha and vascular endothelial growth factor formation. Mol. Cancer Ther., 2003, 2(3), 235-243.
43. Koh, M. Y.; Spivak-Kroizman, T.; Venturini, S.; Welsh, S.; Williams, R. R.; Kirkpatrick, D. L.; Powis, G. Molecular mechanisms for the activity of PX-478, an antitumor inhibitor of the hypoxia-inducible factor-1α. Mol. Cancer Ther., 2008, 7(1), 90-100.
44. Liu, X.; Niu, X.; Zhou, W.; Yi, J. Growth inhibitory effect of β-hydroxyisovalerylshikonin on prostate cancer cells and related mechanism. Journal of Shanghai Jiaotong University (Medical Science), 2010, 30(5), 527-530.
45. Kung, A. L.; Zabludoff, S. D.; France, D. S.; Freedman, S. J.; Tanner, E. A.; Vieira, A.; Cornell-Kennon, S.; Lee, J.; Wang, B.; Wang, J.; Memmert, K.; Naegeli, H. U.; Petersen, F.; Eck, M. J.; Bair, K. W.; Wood, A. W.; Livingston, D. M. Small molecule blockade of transcriptional coactivation of the hypoxia-inducible factor pathway. Cancer Cell, 2004, 6(1), 33-43. (Pubitemid 38903160)
46. Staab, A.; Loeffler, J.; Said, H. M.; Diehlmann, D.; Katzer, A.; Beyer, M.; Fleischer, M.; Schwab, F.; Baier, K.; Einsele, H.; Flentje, M.; Vordermark, D. Effects of HIF-1 inhibition by chetomin on hypoxia-related transcription and radiosensitivity in HT 1080 human fibrosarcoma cells. BMC Cancer, 2007, 7.
47. Kaluz, S.; Kaluzová, M.; Stanbridge, E. J. Proteasomal inhibition attenuates transcriptional activity of hypoxia-inducible factor 1 (HIF-1) via specific effect on the HIF-1α C-terminal activation domain. Mol. Cell. Biol., 2006, 26(15), 5895-5907. (Pubitemid 44134343)
48. Birle, D. C.; Hedley, D. W. Suppression of the hypoxia-inducible factor-1 response in cervical carcinoma xenografts by proteasome inhibitors. Cancer Res., 2007, 67(4), 1735-1743. (Pubitemid 46383400)
49. Semenza, G. L. Evaluation of HIF-1 inhibitors as anticancer agents. Drug Discov. Today, 2007, 12(19-20), 853-859. (Pubitemid 47554628)
50. Newcomb, E. W.; Ali, M. A.; Schnee, T.; Lan, L.; Lukyanov, Y.; Fowkes, M.; Miller, D. C.; Zagzag, D. Flavopiridol downregulates hypoxia-mediated hypoxia-inducible factor-1α expression in human glioma cells by a proteasome-independent pathway: Implications for in vivo therapy. Neuro-Oncology, 2005, 7(3), 225-235. (Pubitemid 41079132)
51. Blagosklonny, M. V. Flavopiridol, an inhibitor of transcription: Implications, problems and solutions. Cell Cycle, 2004, 3(12), 1537-1542. (Pubitemid 40521407)
52. Liu, Y. N.; Pan, S. L.; Peng, C. Y.; Huang, D. Y.; Guh, J. H.; Chen, C. C.; Shen, C. C.; Teng, C. M. Moscatilin repressed lipopolysaccharide-induced hif-1α accumulation and NF-kB activation in murine raw264.7 cells. Shock, 2010, 33(1), 70-75.
53. Jiang, B. H.; Jiang, G.; Zheng, J. Z.; Lu, Z.; Hunter, T.; Vogt, P. K. Phosphatidylinositol 3-kinase signaling controls levels of hypoxia-inducible factor 1. Cell Growth Differ, 2001, 12(7), 4-369.
54. Wang, X. H.; Cavell, B. E.; Syed Alwi, S. S.; Packham, G. Inhibition of hypoxia inducible factor by phenethyl isothiocyanate. Biochem. Pharmacol., 2009, 78(3), 261-272.
55. García-Maceira, P.; Mateo, J. Silibinin inhibits hypoxia-inducible factor-1alpha and mTOR/p70S6K/4E-BP1 signalling pathway in human cervical and hepatoma cancer cells: implications for anticancer therapy. Oncogene, 2009, 28(3), 4-324.
56. Wang, Y.; Xiong, J.; Cheng, H. H.; Zhou, S.; Zhao, Q. Sirolimus inhibits cell proliferation and downregulates mTOR and HIF-1α expression in human hepatic carcinoma HepG2 cells. Shi Jie Hua Ren Xiao Hua Za Zhi, 2009, 17(31), 3241-3243.
57. Wan, X.; Shen, N.; Mendoza, A.; Khanna, C.; Helman, L. J. CCI-779 inhibits rhabdomyosarcoma xenograft growth by an antiangiogenic mechanism linked to the targeting of mTOR/Hif-1α/VEGF signaling. Neoplasia, 2006, 8(5), 394-401. (Pubitemid 43830746)
58. Cejka, D.; Preusser, M.; Woehrer, A.; Sieghart, W.; Strommer, S.; Werzowa, J.; Fuereder, T.; Wacheck, V. Everolimus (RAD001) and anti-angiogenic cyclophosphamide show long-term control of gastric cancer growth in vivo. Cancer Biol. Ther., 2008, 7(9), 1379-1387.
59. Jin, X.; Jin, H. R.; Lee, D.; Lee, J. H.; Kim, S. K.; Lee, J. J. A quassinoid 6atigloyloxychaparrinone inhibits hypoxia-inducible factor-1 pathway by inhibition of eukaryotic translation initiation factor 4E phosphorylation. Euur. J. Pharmacol., 2008, 592(1-3), 41-47.
60. Tang, X. D.; Zhou, X.; Zhou, K. Y. Dauricine inhibits insulin-like growth factor-I-induced hypoxia inducible factor 1α protein accumulation and vascular endothelial growth factor expression in human breast cancer cells. Acta Pharmacol Sin, 2009, 30(5), 605-616.
61. Jeong, J. H.; Jee, Y. A.; Yong, T. K.; Li, L. Y.; Lee, Y. J. Quercetin-induced ubiquitination and down-regulation of Her-2/neu. J. Cell. Biochem., 2008, 105(2), 585-595.
62. Ban, H. S.; Uno, M.; Nakamura, H. Suppression of hypoxia-induced HIF-1α accumulation by VEGFR inhibitors: Different profiles of AAL993 versus SU5416 and KRN633. Cancer Lett., 2010, 296(1), 17-26.
63. Rho, J. K.; Choi, Y. J.; Lee, J. K.; Ryoo, B. Y.; Na, I. I.; Yang, S. H.; Kim, C. H.; Yoo, Y. D.; Lee, J. C. Gefitinib circumvents hypoxia-induced drug resistance by the modulation of HIF-1α. Oncol. Rep., 2009, 21(3), 801-807.
64. Pore, N.; Jiang, Z.; Gupta, A.; Cerniglia, G.; Kao, G. D.; Maity, A. EGFR tyrosine kinase inhibitors decrease VEGF expression by both hypoxiainducible factor (HIF)-1-independent and HIF-1-dependent mechanisms. Cancer Res., 2006, 66(6), 3197-3204.
65. Jin, T.; Nakatani, H.; Taguchi, T.; Nakano, T.; Okabayashi, T.; Sugimoto, T.; Kobayashi, M.; Araki, K. STI571 (Glivec) suppresses the expression of vascular endothelial growth factor in the gastrointestinal stromal tumor cell line, GIST-T1. World J. Gastroenterol., 2006, 12(5), 703-708. (Pubitemid 43380751)
66. Kimura, Y.; Inoue, K.; Abe, M.; Nearman, J.; Baranowska-Kortylewicz, J. PDGFRβ. and HIF-1α inhibition with imatinib and radioimmunotherapy of experimental prostate cancer. Cancer Biol. Ther., 2007, 6(11), 1763-1772. (Pubitemid 351590311)
67. Litz, J.; Krystal, G. W. Imatinib inhibits c-Kit-induced hypoxia-inducible factor-1α activity and vascular endothelial growth factor expression in small cell lung cancer cells. Mol. Cancer Ther., 2006, 5(6), 1415-1422. (Pubitemid 44070477)
68. Luwor, R B.; Lu, Y.; Li, X.; Mendelsohn, J.; Fan, Z. The antiepidermal growth factor receptor monoclonal antibody cetuximab/C225 reduces hypoxia-inducible factor-1 alpha, leading to transcriptional inhibition of vascular endothelial growth factor expression. Oncogene, 2005, 24(27), 4433-4441. (Pubitemid 40961766)
69. Luo, H. Y.; Wei, W.; Shi, Y. X.; Chen, X. Q.; Li, Y. H.; Wang, F.; Qiu, M. Z.; Li, F. H.; Yan, S. L.; Zeng, M. S.; Huang, P.; Xu, R. H. Cetuximab enhances the effect of oxaliplatin on hypoxic gastric cancer cell lines. Oncol. Rep., 2010, 23(6), 1735-1745.
70. Koukourakis, M. I.; Simopoulos, C.; Polychronidis, A.; Perente, S.; Botaitis, S.; Giatromanolaki, A.; Sivridis, E. The effect of trastuzumab/docatexel combination on breast cancer angiogenesis: Dichotomus effect predictable by the HIFIα/VEGF pre-treatment status? Anticancer Res., 2003, 23(2 C), 1673-1680. (Pubitemid 36750829)
71. Pore, N.; Gupta, A. K.; Cerniglia, G. J.; Maity, A. HIV protease inhibitors decrease VEGF/HIF-1αexpression and angiogenesis in glioblastoma cells. Neoplasia, 2006, 8(11), 889-892. (Pubitemid 44706238)
72. Liu, Y. N.; Pan, S. L.; Liao, C. H.; Huang, D. Y.; Guh, J. H.; Peng, C. Y.; Chang, Y. L.; Teng, C. M. Evodiamine represses hypoxia-induced inflammatory proteins expression and hypoxia-inducible factor 1α accumulation in RAW264.7. Shock, 2009, 32(3), 263-269.
73. Tan, C.; De Noronha, R G.; Roecker, A. J.; Pyrzynska, B.; Khwaja, F.; Zhang, Z.; Zhang, H.; Teng, Q.; Nicholson, A. C.; Giannakakou, P.; Zhou, W.; Olson, J. J.; Pereira, M. M.; Nicolaou, K. C.; Van Meir, E. G. Identification of a novel small-molecule inhibitor of the hypoxia-inducible factor 1 pathway. Cancer Res., 2005, 65(2), 605-612.
74. Rapisarda, A.; Uranchimeg, B.; Scudiero, D. A.; Selby, M.; Sausville, E. A.; Shoemaker, R. H.; Melillo, G. Identification of small molecule inhibitors of hypoxia-inducible factor 1 transcriptional activation pathway. Cancer Res., 2002, 62(15), 4316-4324. (Pubitemid 34827288)
75. Zhang, N.; Zhang, H.; Xia, L.; Zheng, Y.; Yu, Y.; Zhu, Y.; Chen, G.; Di, W. NSC606985 induces apoptosis, exerts synergistic effects with cisplatin, and inhibits hypoxia-stabilized HIF-1α protein in human ovarian cancer cells. Cancer Lett., 2009, 278(2), 139-144.
76. Meng, F.; Nguyen, X. T.; Cai, X.; Duan, J.; Matteucci, M.; Hart, C. P. ARC-111 inhibits hypoxia-mediated hypoxia-inducible factor-1α accumulation. Anti-Cancer Drugs, 2007, 18(4), 4-445.
77. Creighton-Gutteridge, M.; Cardellina II, J. H.; Stephen, A. G.; Rapisarda, A.; Uranchimeg, B.; Hite, K.; Denny, W. A.; Shoemaker, R H.; Melillo, G. Cell type-specific, topoisomerase II-dependent inhibition of hypoxia-inducible factor-1α protein accumulation by NSC 644221. Clin. Cancer. Res., 2007, 13(3), 1010-1018. (Pubitemid 46340380)
78. Mabjeesh, N. J.; Escuin, D.; LaVallee, T. M.; Pribluda, V S.; Swartz, G. M.; Johnson, M. S.; Willard, M. T.; Zhong, H.; Simons, J. W.; Giannakakou, P. 2ME2 inhibits tumor growth and angiogenesis by disrupting microtubules and dysregulating HIF. Cancer Cell, 2003, 3(4), 363-375. (Pubitemid 38340305)
79. Mun, J.; Wang, Y.; Voll, R J.; Escuin-Borras, D.; Giannakakou, P.; Goodman, M. M. Syntheses and biological activities of novel 2-methoxyestradiol analogs, 2-flu oroethoxy estradiol and 2-fluoropropanoxyestradiol, and a radiosynthesis of 2-[18F] fluoroethoxyestradiol for positron emission tomography. Nucl. Med. Biol., 2008, 35(5), 615-622. (Pubitemid 351853432)
80. Moser, C.; Lang, S. A.; Mori, A.; Hellerbrand, C.; Schlitt, H. J.; Geissler, E. K.; Fogler, W. E.; Stoeltzing, O. ENMD-1198, a novel tubulin-binding agent reduces HIF-1alpha and STAT3 activity in human hepatocellular carcinoma (HCC) cells, and inhibits growth and vascularization in vivo. BMC Cancer, 2008, 8.
81. LaVallee, T. M.; Burke, P. A.; Swartz, G. M.; Hamel, E.; Agoston, G. E.; Shah, J.; Suwandi, L.; Hanson, A. D.; Fogler, W. E.; Sidor, C. F.; Treston, A. M. Significant antitumor activity in vivo following treatment with the microtubule agent ENMD-1198. Mol. Cancer Ther., 2008, 7(6), 1472-1482.
82. Jun, H. O.; Kim, Y.; Kwon, Y. W.; Hong, S. S.; Kim, K. W.; Shin, J.; Kim, T. Y. Wondonin, a novel compound, inhibits hypoxia-induced angiogenesis through hypoxia-inducible factor 1 alpha. FEBS Lett., 2007, 581(25), 4977-4982. (Pubitemid 47542269)
83. Zhang, Q.; Tang, X.; Lu, Q.; Zhang, Z.; Rao, J.; Le, A. D. Green tea extract and (-)-epigallocatechin-3-gallate inhibit hypoxia-and serum-induced HIF-1protein accumulation and VEGF expression in human cervical carcinoma and hepatoma cells. Mol. Cancer Ther., 2006, 5(5), 1227-1238. (Pubitemid 43881315)
84. Liu, Y.; Liu, R.; Mao, S. C.; Morgan, J. B.; Jekabsons, M. B.; Zhou, Y. D.; Nagle, D. G. Molecular-targeted antitumor agents. 19. Furospongolide from a marine Lendenfeldia sp. sponge inhibits hypoxia-inducible factor-1 activation in breast tumor cells. J. Nat. Prod., 2008, 71(11), 1854-1860.
85. 2-scavenging effect. Mol. Cancer Ther., 2009, 8(10), 2791-2802.
86. Choi, H.; Chun, Y. S.; Kim, S. W.; Kim, M. S.; Park, J. W. Curcumin inhibits hypoxia-inducible factor-1 by degrading aryl hydrocarbon receptor nuclear translocator: A mechanism of tumor growth inhibition. Mol. Pharmacol., 2006, 70(5), 1664-1671.
87. Thomas, S. L.; Zhong, D.; Zhou, W.; Malik, S.; Liotta, D.; Snyder, J. P.; Hamel, E.; Giannakakou, P. EF24, a novel curcumin analog, disrupts the microtubule cytoskeleton and inhibits HIF-1. Cell Cycle, 2008, 7(15), 2409-2417.
88. Park, S. Y.; Jeong, K. J.; Lee, J.; Yoon, D. S.; Choi, W. S.; Kim, Y. K.; Han, J. W.; Kim, Y. M.; Kim, B. K.; Lee, H. Y. Hypoxia enhances LPA-induced HIF-1α and VEGF expression: Their inhibition by resveratrol. Cancer Lett., 2007, 258(1), 63-69. (Pubitemid 47600493)
89. Zhang, Q.; Tang, X.; Lu, Q. Y.; Zhang, Z. F.; Brown, J.; Le, A. D. Resveratrol inhibits hypoxia-induced accumulation of hypoxia-inducible factor-1α and VEGF expression in human tongue squamous cell carcinoma and hepatoma cells. Mol. Cancer Ther., 2005, 4(10), 1465-1474. (Pubitemid 41556428)
90. Kurebayashi, J.; Otsuki, T.; Kurosumi, M.; Soga, S.; Akinaga, S.; Sonoo, H. A radicicol derivative, KF58333, inhibits expression of hypoxia-inducible factor-1α and vascular endothelial growth factor, angiogenesis and growth of human breast cancer xenografts. Jap. J. Cancer Res., 2001, 92(12), 1342-1351. (Pubitemid 34036899)
91. Lang, S. A.; Moser, C.; Gaumann, A.; Klein, D.; Glockzin, G.; Popp, F. C.; Dahlke, M. H.; Piso, P.; Schlitt, H. J.; Geissler, E. K.; Stoeltzing, O. Targeting heat shock protein 90 in pancreatic cancer impairs insulin-like growth factor-I receptor signaling, disrupts an interleukin-6/signal-transducer and activator of transcription 3/hypoxia-inducible factor-1α autocrine loop, and reduces orthotopic tumor growth. Clin. Cancer. Res., 2007, 13(21), 6459-6468. (Pubitemid 350075036)
92. Lancet, J. E.; Gojo, I.; Burton, M.; Quinn, M.; Tighe, S. M.; Kersey, K.; Zhong, Z.; Albitar, M. X.; Bhalla, K.; Hannah, A. L.; Baer, M. R. Phase I study of the heat shock protein 90 inhibitor alvespimycin (KOS-1022, 17-DMAG) administered intravenously twice weekly to patients with acute myeloid leukemia. Leukemia, 2010, 24(4), 699-705.
93. Oh, S. H.; Woo, J. K.; Yazici, Y. D.; Myers, J. N.; Kim, W. Y.; Jin, Q.; Hong, S. S.; Park, H. J.; Suh, Y. G.; Kim, K. W.; Hong, W. K.; Lee, H. Y. Structural basis for depletion of heat shock protein 90 client proteins by deguelin. J. Natl. Cancer Inst., 2007, 99(12), 949-961. (Pubitemid 47073501)
94. Kim, W. Y.; Oh, S. H.; Woo, J. K.; Hong, W. K.; Lee, H. Y. Targeting heat shock protein 90 overrides the resistance of lung cancer cells by blocking radiation-induced stabilization of hypoxia-inducible factor-1α. Cancer Res., 2009, 69(4), 1624-1632.
95. Eccles, S. A.; Massey, A.; Raynaud, F. I.; Sharp, S. Y.; Box, G.; Valenti, M.; Patterson, L.; Brandon, A. D. H.; Gowan, S.; Boxall, F.; Aherne, W.; Rowlands, M.; Hayes, A.; Martins, V.; Urban, F.; Boxall, K.; Prodromou, C.; Pearl, L.; James, K.; Matthews, T. P.; Cheung, K. M.; Kalusa, A.; Jones, K.; McDonald, E.; Barril, X.; Brough, P. A.; Cansfield, J. E.; Dymock, B.; Drysdale, M. J.; Finch, H.; Howes, R.; Hubbard, R. E.; Surgenor, A.; Webb, P.; Wood, M.; Wright, L.; Workman, P. NVP-AUY922: A novel heat shock protein 90 inhibitor active against xenograft tumor growth, angiogenesis, and metastasis. Cancer Res., 2008, 68(8), 2850-2860. (Pubitemid 351556284)
96. Gaspar, N.; Sharp, S. Y.; Eccles, S. A.; Gowan, S.; Popov, S.; Jones, C.; Pearson, A.; Vassal, G.; Workman, P. Mechanistic evaluation of the novel HSP90 inhibitor NVP-AUY922 in adult and pediatric glioblastoma. Mol. Cancer Ther., 2010, 9(5), 1219-1233.
97. Li, Z. D.; Liu, L. Z.; Shi, X.; Fang, J.; Jiang, B. H. Benzo[a]pyrene-3, 6-dione inhibited VEGF expression through inducing HIF-1α degradation. BBRC, 2007, 357(2), 517-523. (Pubitemid 46603161)
98. Won, M. S.; Im, N.; Park, S.; Boovanahalli, S. K.; Jin, Y.; Jin, X.; Chung, K. S.; Kang, M.; Lee, K.; Park, S. K.; Kim, H. M.; Kwon, B. M.; Lee, J. J. A novel benzimidazole analogue inhibits the hypoxia-inducible factor (HIF)-1 pathway. BBRC, 2009, 385(1), 16-21.
99. Lee, K.; Kang, J. E.; Park, S. K.; Jin, Y.; Chung, K. S.; Kim, H. M.; Kang, M. R.; Lee, M. K.; Song, K. B.; Yang, E. G.; Lee, J. J.; Won, M. LW6, a novel HIF-1 inhibitor, promotes proteasomal degradation of HIF-1α via upregulation of VHL in a colon cancer cell line. Biochem. Pharmacol., 2010.
100. Yang, Q. C.; Zeng, B. F.; Shi, Z. M.; Dong, Y.; Jiang, Z. M.; Huang, J.; Lv, Y. M.; Yang, C. X.; Liu, Y. W. Inhibition of hypoxia-induced angiogenesis by trichostatin A via suppression of HIF-1α activity in human osteosarcoma. J. Exp. Clin. Cancer Res., 2006, 25(4), 593-599. (Pubitemid 46170683)
101. Qian, D. Z.; Kachhap, S. K.; Collis, S. J.; Verheul, H. M. W.; Carducci, M. A.; Atadja, P.; Pili, R. Class II histone deacetylases are associated with VHL-independent regulation of hypoxia-inducible factor 1α. Cancer Res., 2006, 66(17), 8814-8821. (Pubitemid 44449199)
102. Shankar, S.; Davis, R.; Singh, K. P.; Kurzrock, R.; Ross, D. D.; Srivastava, R. K. Suberoylanilide hydroxamic acid (Zolinza/vorinostat) sensitizes TRAIL-resistant breast cancer cells orthotopically implanted in BALB/c nude mice. Mol. Cancer Ther., 2009, 8(6), 1596-1605.
103. Lee, Y. M.; Kim, S. H.; Kim, H. S.; Son, M. J.; Nakajima, H.; Kwon, H. J.; Kim, K. W. Inhibition of hypoxia-induced angiogenesis by FK228, a specific histone deacetylase inhibitor, via suppression of HIF-1α activity. BBRC, 2003, 300(1), 241-246. (Pubitemid 36042959)
104. Durczak, M.; Jagodzinski, P. P. Apicidin upregulates PHD2 prolyl hydroxylase gene expression in cervical cancer cells. Anti-Cancer Drugs, 2010, 21(6), 4-624.
105. Han, J. Y.; Oh, S. H.; Morgillo, F.; Myers, J. N.; Kim, E.; Hong, W. K.; Lee, H. Y. Hypoxia-inducible factor 1α and antiangiogenic activity of farnesyltransferase inhibitor SCH66336 in human aerodigestive tract cancer. J. Natl. Cancer Inst., 2005, 97(17), 1272-1286. (Pubitemid 41535368)
106. Shan, H. L.; Dong, H. S.; Chun, Y. S.; Myung, K. L.; Kim, M. S.; Park, J. W. A novel mode of action of YC-1 in HIF inhibition: Stimulation of FIH-dependent p300 dissociation from HIF-1α. Mol. Cancer Ther., 2008, 7(12), 3729-3738.
107. Sun, H. L.; Liu, Y. N.; Huang, Y. T.; Pan, S. L.; Huang, D. Y.; Guh, J. H.; Lee, F. Y.; Kuo, S. C.; Teng, C. M. YC-1 inhibits HIF-1 expression in prostate cancer cells: Contribution of Akt/NF-κB signaling to HIF-1α accumulation during hypoxia. Oncogene, 2007, 26(27), 4-3951.
108. Zhong, H.; Willard, M.; Simons, J. NS398 reduces hypoxia-inducible factor (HIF)-1α and HIF-1 activity: Multiple-level effects involving cyclooxygenase-2 dependent and independent mechanisms. Int. J. Cancer, 2004, 112(4), 4-595.
109. Palayoor, S. T.; Tofilon, P. J.; Coleman, C. N. Ibuprofen-mediated reduction of hypoxia-inducible factors HIF-1α and HIF-2α in prostate cancer cells. Clin. Cancer Res., 2003, 9(8), 3150-3157. (Pubitemid 37006311)
110. Li, M. H.; Miao, Z. H.; Tan, W. F.; Yue, J. M.; Zhang, C.; Lin, L. P.; Zhang, X. W.; Ding, J. Pseudolaric acid B inhibits angiogenesis and reduces hypoxia-inducible factor 1α by promoting proteasome-mediated degradation. Clin. Cancer. Res., 2004, 10(24), 8266-8274. (Pubitemid 40053386)
111. Lin, S.; Tsai, S. C.; Lee, C. C.; Wang, B. W.; Liou, J. Y.; Shyu, K. G. Berberine inhibits HIF-1α expression via enhanced proteolysis. Mol. Pharmacol., 2004, 66(3), 612-619. (Pubitemid 39329260)
112. Suzuki, M.; Shinohara, F.; Rikiishi, H. Zebularine-induced reduction in VEGF secretion by HIF-1α degradation in oral squamous cell carcinoma. Mol Med Report, 2008, 1(4), 4-471.
113. Ali, M. A.; Reis, A.; Ding, L. H.; Story, M. D.; Habib, A. A.; Chattopadhyay, A.; Saha, D. SNS-032 prevents hypoxia-mediated glioblastoma cell invasion by inhibiting hypoxia inducible factor-1α expression. Int. J. Oncol., 2009, 34(4), 1051-1060.
114. Dal Piaz, F.; Braca, A.; Belisario, M. A.; De Tommasi, N. Thioredoxin system modulation by plant and fungal secondary metabolites. Curr Med. Chem., 2010, 17(5), 479-494.
115. Jung, H. J.; Park, J. W.; Lee, J. S.; Lee, S. R.; Jang, B. C.; Suh, S. I.; Suh, M. H.; Baek, W. K. Silibinin inhibits expression of HIF-1α through suppression of protein translation in prostate cancer cells. BBRC, 2009, 390(1), 71-76.
116. Lin, C. J.; Sukarieh, R.; Pelletier, J. Silibinin inhibits translation initiation: Implications for anticancer therapy. Mol. Cancer Ther., 2009, 8(6), 1606-1612.
117. Triantafyllou, A.; Liakos, P.; Tsakalof, A.; Chachami, G.; Paraskeva, E.; Molyvdas, P. A.; Georgatsou, E.; Simos, G.; Bonanou, S. The flavonoid quercetin induces hypoxia-inducible factor-1α (HIF-1α) and inhibits cell proliferation by depleting intracellular iron. Free Radical Res., 2007, 41(3), 342-356. (Pubitemid 46404478)
118. Radreau, P.; Rhodes, J. D.; Mithen, R. F.; Kroon, P. A.; Sanderson, J. Hypoxia-inducible factor-1 (HIF-1) pathway activation by quercetin in human lens epithelial cells. EEyeR, 2009, 89(6), 995-1002.
119. Park, S. S.; Bae, I.; Lee, Y. J. Flavonoids-induced accumulation of hypoxiainducible factor (HIF)-1α/2α is mediated through chelation of iron. J. Cell. Biochem., 2008, 103(6), 1989-1998. (Pubitemid 351501927)
120. Triantafyllou, A.; Mylonis, I.; Simos, G.; Bonanou, S.; Tsakalof, A. Flavonoids induce HIF-1α but impair its nuclear accumulation and activity. Free Radical Biol. Med., 2008, 44(4), 657-670.
121. Wang, G. L.; Semenza, G. L. Desferrioxamine induces erythropoietin gene expression and hypoxia-inducible factor 1 DNA-binding activity: Implications for models of hypoxia signal transduction. Blood, 1993, 82(12), 3610-3615. (Pubitemid 24006041)
122. Ansó, E.; Zuazo, A.; Irigoyen, M.; Urdaci, M. C.; Rouzaut, A.; Martínez-Irujo, J. J. Flavonoids inhibit hypoxia-induced vascular endothelial growth factor expression by a HIF-1 independent mechanism. Biochem. Pharmacol., 2010, 79(11), 1600-1609.
123. Lee, D. H.; Lee, Y. J. Quercetin suppresses hypoxia-induced accumulation of hypoxia-inducible factor-1α (HIF-1α) through inhibiting protein synthesis. J. Cell. Biochem., 2008, 105(2), 546-553.
124. Du, G.; Lin, H.; Wang, M.; Zhang, S.; Wu, X.; Lu, L.; Ji, L.; Yu, L. Quercetin greatly improved therapeutic index of doxorubicin against 4T1 breast cancer by its opposing effects on HIF-1α in tumor and normal cells. Cancer Chemother. Pharmacol., 2010, 65(2), 277-287.
125. Luo, H.; Jiang, B. H.; King, S. M.; Chen, Y. C. Inhibition of cell growth and VEGF expression in ovarian cancer cells by flavonoids. Nutr. Cancer, 2008, 60(6), 800-809.
126. Luo, H.; Rankin, G. O.; Liu, L.; Daddysman, M. K.; Jiang, B. H.; Chen, Y. C. Kaempferol inhibits angiogenesis and VEGF expression through both HIF dependent and independent pathways in human ovarian cancer cells. Nutr. Cancer, 2009, 61(4), 554-563.
127. Mirzoeva, S.; Nam, D. K.; Chiu, K.; Franzen, C. A.; Bergan, R. C.; Pelling, J. C. Inhibition of HIF-1 alpha and VEGF expression by the chemopreventive bioflavonoid apigenin is accompanied by Akt inhibition in human prostate carcinoma PC3-M cells. Mol. Carcinog., 2008, 47(9), 686-700.
128. Choi, H. J.; Eun, J. S.; Kim, B. G.; Kim, S. Y.; Jeon, H.; Soh, Y. Vitexin, an HIF-1α inhibitor, has anti-metastatic potential in PC12 cells. Mol. Cells, 2006, 22(3), 4-299.
129. Luo, W. J.; Wang, G. H.; Zhang, X.; Chen, Z. N.; Wang, N. L.; Yao, X. S. Inhibitory effect of bibenzyls from Dendrobium Nobile on the proliferation of high invasive hepatoma cell line FHCC-98. Chinese Journal of Clinical
130. Lee, J. H.; Lee, D. H.; Lee, H. S.; Choi, J. S.; Kim, K. W.; Hong, S. S. Deguelin inhibits human hepatocellular carcinoma by antiangiogenesis and apoptosis. Oncol. Rep., 2008, 20(1), 129-134.
131. Oh, S. H.; Woo, J. K.; Jin, Q.; Kang, H. J.; Jeong, J. W.; Kim, K. W.; Waun, K. H.; Lee, H. Y. Identification of novel antiangiogenic anticancer activities of deguelin targeting hypoxia-inducible factor-1 alpha. Int. J. Cancer, 2008, 122(1), 5-14. (Pubitemid 350209972)
132. Kim, W. Y.; Chang, D. J.; Hennessy, B.; Kang, H. J.; Yoo, J.; Han, S. H.; Kim, Y. S.; Park, H. J.; Geo, S. Y.; Mills, G.; Kim, K. W.; Hong, W. K.; Suh, Y. G.; Lee, H. Y. A novel derivative of the natural agent deguelin for cancer chemoprevention and therapy. Cancer Prev Res (Phila Pa), 2008, 1(7), 577-587.
133. Harikumar, K. B.; Aggarwal, B. B. Resveratrol: A multitargeted agent for age-associated chronic diseases. Cell Cycle, 2008, 7(8), 1020-1037. (Pubitemid 351679835)
134. Cao, Z.; Fang, J.; Xia, C.; Shi, X.; Jiang, B. H. trans-3, 4, 5'-Trihydroxystibene inhibits hypoxia-inducible factor 1α and vascular endothelial growth factor expression in human ovarian cancer cells. Clin. Cancer. Res., 2004, 10(15), 5253-5263. (Pubitemid 39099800)
135. Wu, H.; Liang, X.; Fang, Y.; Qin, X.; Zhang, Y.; Liu, J. Resveratrol inhibits hypoxia-induced metastasis potential enhancement by restricting hypoxiainduced factor-1α expression in colon carcinoma cells. Biomed. Pharmacother., 2008, 62(9), 613-621.
136. Ban, H. S.; Uno, M.; Nakamura, H. Suppression of hypoxia-induced HIF-1α accumulation by VEGFR inhibitors: Different profiles of AAL993 versus SU5416 and KRN633. Cancer Lett., 2010.
137. Vezina, C.; Kudelski, A.; Sehgal, S. N. Rapamycin (AY 22, 989), a new antifungal antibiotic. I. Taxonomy of the producing streptomycete and isolation of the active principle. J. Antibiot., 1975, 28(10), 721-726.
138. Shor, B.; Gibbons, J. J.; Abraham, R. T.; Yu, K. Targeting mTOR globally in cancer: Thinking beyond rapamycin. Cell Cycle, 2009, 8(23), 3831-3837.
139. Feldman, M. E.; Apsel, B.; Uotila, A.; Loewith, R.; Knight, Z. A.; Ruggero, D.; Shokat, K. M. Active-site inhibitors of mTOR target rapamycin-resistant outputs of mTORC1 and mTORC2. PLoS Biol., 2009, 7(2), 0371-0383.
140. Verma, R. P.; Hansch, C. Camptothecins: A SAR/QSAR study. Chem. Rev., 2009, 109(1), 213-235.
141. Rapisarda, A.; Uranchimeg, B.; Sordet, O.; Pommier, Y.; Shoemaker, R. H.; Melillo, G. Topoisomerase I-Mediated Inhibition of Hypoxia-Inducible Factor 1: Mechanism and Therapeutic Implications. Cancer Res., 2004, 64(4), 1475-1482. (Pubitemid 38235619)
142. Choi, Y. J.; Rho, J. K.; Lee, S. J.; Jang, W. S.; Lee, S. S.; Kim, C. H.; Lee, J. C. HIF-1α modulation by topoisomerase inhibitors in non-small cell lung cancer cell lines. J. Cancer Res. Clin. Oncol., 2009, 135(8), 4-1053.
143. Baranello, L.; Bertozzi, D.; Fogli, M. V.; Pommier, Y.; Capranico, G. DNA topoisomerase I inhibition by camptothecin induces escape of RNA polymerase II from promoter-proximal pause site, antisense transcription and histone acetylation at the human HIF-1α gene locus. NAR, 2009, 38(1), 159-171.
144. Merritt, W. M.; Danes, C. G.; Shahzad, M. M. K.; Lin, Y. G.; Kamat, A. A.; Han, L. Y.; Spannuth, W. A.; Nick, A. M.; Mangala, L. S.; Stone, R. L.; Hye, S. K.; Gershenson, D. M.; Jaffe, R. B.; Coleman, R. L.; Chandra, J.; Sood, A. K. Anti-angiogenic properties of metronomic topotecan in ovarian carcinoma. Cancer Biol. Ther., 2009, 8(16), 1596-1603.
145. Ricker, J. L.; Chen, Z.; Yang, X. P.; Pribluda, V S.; Swartz, G. M.; Van Waes, C. 2-Methoxyestradiol inhibits hypoxia-inducible factor 1α, tumor growth, and angiogenesis and augments paclitaxel efficacy in head and neck squamous cell carcinoma. Clin. Cancer. Res., 2004, 10(24), 8665-8673. (Pubitemid 40053435)
146. Kang, S. H.; Cho, H. T.; Devi, S.; Zhang, Z.; Escuin, D.; Liang, Z.; Mao, H.; Brat, D. J.; Olson, J. J.; Simons, J. W.; LaVallee, T. M.; Giannakakou, P.; Van Meir, E. G.; Shim, H. Antitumor effect of 2-methoxyestradiol in a rat orthotopic brain tumor model. Cancer Res., 2006, 66(24), 11991-11997. (Pubitemid 46094213)
147. James, J.; Murry, D. J.; Treston, A. M.; Storniolo, A. M.; Sledge, G. W.; Sidor, C.; Miller, K. D. Phase I safety, pharmacokinetic and pharmacodynamic studies of 2-methoxyestradiol alone or in combination with docetaxel in patients with locally recurrent or metastatic breast cancer. Invest. New Drugs, 2007, 25(1), 4-48.
148. Sweeney, C.; Liu, G.; Yiannoutsos, C.; Kolesar, J.; Horvath, D.; Staab, M. J.; Fife, K.; Armstrong, V.; Treston, A.; Sidor, C.; Wilding, G. A phase II multicenter, randomized, double-blind, safety trial assessing the pharmacokinetics, pharmacodynamics, and efficacy of oral 2-methoxyestradiol capsules in hormone-refractory prostate cancer. Clin. Cancer. Res., 2005, 11(18), 6625-6633. (Pubitemid 41339003)
149. Chua, Y. S.; Chua, Y. L.; Hagen, T. Structure activity analysis of 2-methoxyestradiol analogues reveals targeting of microtubules as the major mechanism of antiproliferative and proapoptotic activity. Mol. Cancer Ther., 2010, 9(1), 224-235.
150. Jourdan, F.; Leese, M. P.; Dohle, W.; Hamel, E.; Ferrandis, E.; Newman, S. P.; Purohit, A.; Reed, M. J.; Potter, B. V. L. Synthesis, antitubulin, and antiproliferative SAR of analogues of 2-methoxyestradiol-3, 17-O, O-bissulfamate. J. Med. Chem., 2010, 53(7), 2942-2951.
151. Edsall, A. B.; Mohanakrishnan, A. K.; Yang, D.; Fanwick, P. E.; Hamel, E.; Hanson, A. D.; Agoston, G. E.; Cushman, M. Effects of altering the electronics of 2-methoxyestradiol on cell proliferation, on cytotoxicity in human cancer cell cultures, and on tubulin polymerization. J. Med. Chem., 2004, 47(21), 5126-5139. (Pubitemid 39314910)
152. Edsall, A. B.; Agoston, G. E.; Treston, A. M.; Plum, S. M.; McClanahan, R. H.; Lu, T. S.; Song, W.; Cushman, M. Synthesis and in vivo antitumor evaluation of 2-methoxyestradiol 3-phosphate, 17-phosphate, and 3, 17-diphosphate. J. Med. Chem., 2007, 50(26), 6700-6705. (Pubitemid 350309107)
153. Stravopodis, D. J.; Margaritis, L. H.; Voutsinas, G. E. Drug-mediated targeted disruption of multiple protein activities through functional inhibition of the Hsp90 chaperone complex. Curr. Med. Chem., 2007, 14(29), 3122-3138. (Pubitemid 350226961)
154. Tian, Z. Q.; Liu, Y.; Zhang, D.; Wang, Z.; Dong, S. D.; Carreras, C. W.; Zhou, Y.; Rastelli, G.; Santi, D. V.; Myles, D. C. Synthesis and biological activities of novel 17-aminogeldanamycin derivatives. Bioorg. Med. Chem., 2004, 12(20), 5317-5329. (Pubitemid 39243952)
155. Rastelli, G.; Tian, Z. Q.; Wang, Z.; Myles, D.; Liu, Y. Structure-based design of 7-carbamate analogs of geldanamycin. Bioorg. Med. Chem. Lett., 2005, 15(22), 5016-5021. (Pubitemid 41400176)
156. Tian, Z. Q.; Wang, Z.; MacMillan, K. S.; Zhou, Y.; Carreras, C. W.; Mueller, T.; Myles, D. C.; Liu, Y. Potent cytotoxic C-11 modified geldanamycin analogues. J. Med. Chem., 2009, 52(10), 3265-3273.
157. Porter, J. R.; Ge, J.; Lee, J.; Normant, E.; West, K. Ansamycin inhibitors of Hsp90: Nature's prototype for anti-chaperone therapy. Curr. Top. Med. Chem., 2009, 9(15), 1386-1418.
158. Adachi, S.; Yasuda, I.; Nakashima, M.; Yamauchi, T.; Yamauchi, J.; Natsume, H.; Moriwaki, H.; Kozawa, O. HSP90 inhibitors induce desensitization of EGF receptor via p38 MAPK-mediated phosphorylation at Ser1046/1047 in human pancreatic cancer cells. Oncol. Rep., 2010, 23(6), 1709-1714.
159. Ferrario, A.; Gomer, C. J. Targeting the 90 kDa heat shock protein improves photodynamic therapy. Cancer Lett., 2010, 289(2), 188-194.
160. Ellis, L.; Hammers, H.; Pili, R. Targeting tumor angiogenesis with histone deacetylase inhibitors. Cancer Lett., 2009, 280(2), 145-153.
161. Kong, X.; Lin, Z.; Liang, D.; Fath, D.; Sang, N.; Caro, J. Histone deacetylase inhibitors induce VHL and ubiquitin-in dependent proteasomal degradation of hypoxia-inducible factor 1α. Mol. Cell. Biol., 2006, 26(6), 4-2028.
162. Kim, S. H.; Jeong, J. W.; Park, J. A.; Lee, J. W.; Seo, J. H.; Jung, B. K.; Bae, M. K.; Kim, K. W. Regulation of the HIF-1alpha stability by histone deacetylases. Oncol. Rep., 2007, 17(3), 647-651.
163. Seo, H. W.; Kim, E. J.; Na, H.; Lee, M. O. Transcriptional activation of hypoxia-inducible factor-1α by HDAC4 and HDAC5 involves differential recruitment of p300 and FIH-1. FEBS Lett., 2009, 583(1), 55-60.
164. Witt, O.; Deubzer, H. E.; Milde, T.; Oehme, I. HDAC family: What are the cancer relevant targets? Cancer Lett., 2009, 277(1), 8-21.
165. De Bono, J. S.; Kristeleit, R.; Tolcher, A.; Fong, P.; Pacey, S.; Karavasilis, V.; Mita, M.; Shaw, H.; Workman, P.; Kaye, S.; Rowinsky, E. K.; Aherne, W.; Atadja, P.; Scott, J. W.; Patnaik, A. Phase I pharmacokinetic and pharmacodynamic study of LAQ824, a hydroxamate histone deacetylase inhibitor with a heat shock protein-90 inhibitory profile, in patients with advanced solid tumors. Clin. Cancer. Res., 2008, 14(20), 6663-6673.
166. Richon, V M.; Garcia-Vargas, J.; Hardwick, J. S. Development of vorinostat: Current applications and future perspectives for cancer therapy. Cancer Lett., 2009, 280(2), 201-210.
167. Mahalingam, D.; Medina, E. C.; Esquivel II, J. A.; Espitia, C. M.; Smith, S.; Oberheu, K.; Swords, R.; Kelly, K. R.; Mita, M. M.; Mita, A. C.; Carew, J. S.; Giles, F. J.; Nawrocki, S. T. Vorinostat enhances the activity of temsirolimus in renal cell carcinoma through suppression of survivin levels. Clin. Cancer. Res., 2010, 16(1), 141-153.
168. Nielsen, T. O.; Nguyen, A.; Su, L.; Campbell, B.; Poulin, N. M. Synergism of heat shock protein 90 and histone deacetylase inhibitors in synovial sarcoma. Sarcoma, 2009, 2009.
169. Lin, Z.; Bazzaro, M.; Wang, M. C.; Chan, K. C.; Peng, S.; Roden, R. B. S. Combination of proteasome and HDAC inhibitors for uterine cervical cancer treatment. Clin. Cancer. Res., 2009, 15(2), 570-577.
170. Cho, Y. S.; Whitehead, L.; Li, J.; Chen, C. H. T.; Jiang, L.; Vögtle, M.; Francotte, E.; Richert, P.; Wagner, T.; Traebert, M.; Lu, Q.; Cao, X.; Dumotier, B.; Fejzo, J.; Rajan, S.; Wang, P.; Yan-Neale, Y.; Shao, W.; Atadja, P.; Shultz, M. Conformational refinement of hydroxamate-based histone deacetylase inhibitors and exploration of 3-piperidin-3-ylindole analogues of dacinostat (LAQ824). J. Med. Chem., 2010, 53(7), 2952-2963.
171. Lee, K.; Lee, J. H.; Boovanahalli, S. K.; Jin, Y.; Lee, M.; Jin, X.; Kim, J. H.; Hong, Y. S.; Lee, J. J. (Aryloxyacetylamino) benzoic acid analogues: A new class of hypoxia-inducible factor-1 inhibitors. J. Med. Chem., 2007, 50(7), 1675-1684. (Pubitemid 46564388)
172. Boovanahalli, S. K.; Jin, X.; Jin, Y.; Kim, J. H.; Dat, N. T.; Hong, Y. S.; Lee, J. H.; Jung, S. H.; Lee, K.; Lee, J. J. Synthesis of (aryloxyacetylamino) - isonicotinic/nicotinic acid analogues as potent hypoxia-inducible factor (HIF)-1α inhibitors. Bioorg. Med. Chem. Lett., 2007, 17(22), 6305-6310. (Pubitemid 47552815)
173. Hu, J.; Straub, J.; Xiao, D.; Singh, S. V.; Yang, H. S.; Sonenberg, N.; Vatsyayan, J. Phenethyl isothiocyanate, a cancer chemopreventive constituent of cruciferous vegetables, inhibits cap-dependent translation by regulating the level and phosphorylation of 4E-BP1. Cancer Res., 2007, 67(8), 3569-3573. (Pubitemid 46762140)
174. Tong, W. G.; Chen, R.; Plunkett, W.; Siegel, D.; Sinha, R.; Harvey, R D.; Badros, A. Z.; Popplewell, L.; Coutre, S.; Fox, J. A.; Mahadocon, K.; Chen, T.; Kegley, P.; Hoch, U.; Wierda, W. G. Phase I and pharmacologic study of SNS-032, a potent and selective Cdk 2, 7, and 9 inhibitor, in patients with advanced chronic lymphocytic leukemia and multiple myeloma. J. Clin. Oncol., 2010, 28(18), 4-3022.
175. Murugan, R S.; Vinothini, G.; Hara, Y.; Nagini, S. Black tea polyphenols target matrix metalloproteinases, RECK, proangiogenic molecules and histone deacetylase in a rat hepatocarcinogenesis model. Anticancer Res., 2009, 29(6), 2301-2305.
176. Chau, N. M.; Rogers, P.; Aherne, W.; Carroll, V.; Collins, I.; McDonald, E.; Workman, P.; Ashcroft, M. Identification of novel small molecule inhibitors of hypoxia-inducible factor-1 that differentially block hypoxia-inducible factor-1 activity and hypoxia-inducible factor-1α induction in response to hypoxic stress and growth factors. Cancer Res., 2005, 65(11), 4918-4928. (Pubitemid 40740832)
177. Mohammed, K. A.; Hossain, C. F.; Zhang, L.; Bruick, R K.; Zhou, Y. D.; Nagle, D. G. Laurenditerpenol, a new diterpene from the tropical marine alga Laurencia intricata that potently inhibits HIF-1 mediated hypoxic signaling in breast tumor cells. J. Nat. Prod., 2004, 67(12), 2002-2007. (Pubitemid 40092545)
178. Athinaios, N.; Kazantzis, A.; Putzker, K.; Lewis, J.; Pitsinos, E. N. Synthesis of Novel laurenditerpenol analogues and their evaluation as HIF-1 activation inhibitors. Lett Org Chem, 2009, 6(4), 269-271.
179. El Sayed, K. A.; Khanfar, M. A.; Shallal, H. M.; Muralidharan, A.; Awate, B.; Youssef, D. T. A.; Liu, Y.; Zhou, Y. D.; Nagle, D. G.; Shah, G. Latrunculin A and its C-17-O-carbamates inhibit prostate tumor cell invasion and HIF-1 activation in breast tumor cells. J. Nat. Prod., 2008, 71(3), 396-402. (Pubitemid 351549362)
180. Straight, A. M.; Oakley, K.; Moores, R.; Bauer, A. J.; Patel, A.; Tuttle, R. M.; Jimeno, J.; Francis, G. L. Aplidin reduces growth of anaplastic thyroid cancer xenografts and the expression of several angiogenic genes. Cancer Chemother. Pharmacol., 2006, 57(1), 7-14. (Pubitemid 41704919)
181. Mohammed, K. A.; Jadulco, R C.; Bugni, T. S.; Harper, M. K.; Sturdy, M.; Ireland, C. M. Strongylophorines: Natural product inhibitors of hypoxiainducible factor-1 transcriptional pathway. J. Med. Chem., 2008, 51(5), 1402-1405. (Pubitemid 351480401)
182. Dai, J.; Fishback, J. A.; Zhou, Y. D.; Nagle, D. G. Sodwanone and yardenone triterpenes from a South African species of the marine sponge Axinella inhibit hypoxia-inducible factor-1 (HIF-1) activation in both breast and prostate tumor cells. J. Nat. Prod., 2006, 69(12), 1715-1720. (Pubitemid 46144964)
183. Wu, C. Z.; Cai, X. F.; Dat, N. T.; Hong, S. S.; Han, A. R.; Seo, E. K.; Hwang, B. Y.; Nan, J. X.; Lee, D.; Lee, J. J. Bisbakuchiols A and B, novel dimeric meroterpenoids from Psoralea corylifolia. Tetrahedron Lett., 2007, 48(50), 8861-8864. (Pubitemid 350088043)
184. Wu, C. Z.; Hong, S. S.; Cai, X. F.; Dat, N. T.; Nan, J. X.; Hwang, B. Y.; Lee, J. J.; Lee, D. Hypoxia-inducible factor-1 and nuclear factor-KB inhibitory meroterpene analogues of bakuchiol, a constituent of the seeds of Psoralea corylifolia. Bioorg. Med. Chem. Lett., 2008, 18(8), 2619-2623. (Pubitemid 351503880)
185. Warabi, K.; McHardy, L. M.; Matainaho, L.; Van Soest, R.; Roskelley, C. D.; Roberge, M.; Andersen, R J. Strongylophorine-26, a new meroditerpertoid isolated from the marine sponge Petrosia (Strongylophora) corticata that exhibits anti-invasion activity. J. Nat. Prod., 2004, 67(8), 1387-1389. (Pubitemid 39145647)
186. Warabi, K.; Patrick, B. O.; Austin, P.; Roskelley, C. D.; Roberge, M.; Andersen, R J. Strongylophorine-26, an inhibitor of cancer cell invasion: SAR revealed by synthesis of analogues. J. Nat. Prod., 2007, 70(5), 736-740. (Pubitemid 46953591)
187. Monti, E.; Gariboldi, M. B. HIF-1 as a target for cancer chemotherapy, chemosensitization and chemoprevention. Curr. Mol. Pharmacol., 2011, 4(1), 62-77.