메뉴 건너뛰기




Volumn 2, Issue 10, 2010, Pages 1577-1589

Recent advances in the discovery of small molecule mTOR inhibitors

Author keywords

[No Author keywords available]

Indexed keywords

1H PYRAZOLO[3,4 D]PYRIMIDINE; 4 (PYRIDO[2,3 D]PYRIMIDINE 4 YL)MORPHOLINE; AP 23841; AP 24170; BC 210; BIS MORPHOLINO TRIAZINE; DEFOROLIMUS; ENDEAVOR; EVEROLIMUS; FK 506 BINDING PROTEIN; MAMMALIAN TARGET OF RAPAMYCIN INHIBITOR; PHOSPHATIDYLINOSITOL 3 KINASE; PROTEIN KINASE B; RAPAMYCIN; RIDAFOROLIMUS; TEMSIROLIMUS; TRIMAXX; UNCLASSIFIED DRUG; ZOMAXX; ZOTAROLIMUS;

EID: 77958071860     PISSN: 17568919     EISSN: None     Source Type: Journal    
DOI: 10.4155/fmc.10.233     Document Type: Review
Times cited : (14)

References (61)
  • 1
    • 24944480788 scopus 로고    scopus 로고
    • The Akt-mTOR tango and its relevance to cancer
    • Hay N. The Akt-mTOR tango and its relevance to cancer. Cancer Cell 8, 179-183 (2005
    • (2005) Cancer Cell , vol.8 , pp. 179-183
    • Hay, N.1
  • 2
    • 33746637660 scopus 로고    scopus 로고
    • Current development of mTOR inhibitors as anticancer agents
    • Faivre S, Kroemer G, Raymond E. Current development of mTOR inhibitors as anticancer agents. Nat. Rev. Drug Discov. 5, 671-688 (2006
    • (2006) Nat. Rev. Drug Discov. , vol.5 , pp. 671-688
    • Faivre, S.1    Kroemer, G.2    Raymond, E.3
  • 3
    • 57449111076 scopus 로고    scopus 로고
    • MTOR pathway and mTOR inhibitors as agents for cancer therapy
    • Baldo P, Cecco S, Giacomin E et al. mTOR pathway and mTOR inhibitors as agents for cancer therapy. Curr. Cancer Drug Targets 8, 647-665 (2008
    • (2008) Curr. Cancer Drug Targets , vol.8 , pp. 647-665
    • Baldo, P.1    Cecco, S.2    Giacomin, E.3
  • 4
    • 2342545519 scopus 로고    scopus 로고
    • Target of rapamycin (TOR): An integrator of nutrient and growth factor signals and coordinator of cell growth and cell cycle progression
    • Fingar DC, Blenis J. Target of rapamycin (TOR): an integrator of nutrient and growth factor signals and coordinator of cell growth and cell cycle progression. Oncogene 23, 3151-3171(2004
    • (2004) Oncogene , vol.23 , pp. 3151-3171
    • Fingar, D.C.1    Blenis, J.2
  • 5
    • 34347220473 scopus 로고    scopus 로고
    • Defining the role of mTOR in cancer
    • Guertin DA, Sabatini DM. Defining the role of mTOR in cancer. Cancer Cell 12, 9-22 (2007
    • (2007) Cancer Cell , vol.12 , pp. 9-22
    • Guertin, D.A.1    Sabatini, D.M.2
  • 6
    • 23144467910 scopus 로고    scopus 로고
    • An expanding role for mTOR in cancer
    • Guertin DA, Sabatini DM. An expanding role for mTOR in cancer. Trends Mol. Med. 11, 353-361 (2005
    • (2005) Trends Mol. Med. , vol.11 , pp. 353-361
    • Guertin, D.A.1    Sabatini, D.M.2
  • 9
    • 34247253340 scopus 로고    scopus 로고
    • Gene expression profiling of LPS-stimulated murine macrophages and role of the NF-kB and PI3K/mTOR signaling pathways
    • Dos Santos S, Delattre AI, De Longueville F et al. Gene expression profiling of LPS-stimulated murine macrophages and role of the NF-kB and PI3K/mTOR signaling pathways. Ann. N.Y. Acad. Sci. 1096, 70-77 (2007
    • (2007) Ann. N.Y. Acad. Sci. , vol.1096 , pp. 70-77
    • Dos Santos, S.1    Delattre, A.I.2    De Longueville, F.3
  • 10
    • 0033812537 scopus 로고    scopus 로고
    • Phosphatidylinositol 3-kinase and mTOR mediate lipopolysaccharide- stimulated nitric oxide production in macrophages via interferon-b
    • Weinstein SL, Finn AJ, Dave SH et al. Phosphatidylinositol 3-kinase and mTOR mediate lipopolysaccharide-stimulated nitric oxide production in macrophages via interferon-b. J. Leukoc. Biol. 67, 405-414 (2000
    • (2000) J. Leukoc. Biol. , vol.67 , pp. 405-414
    • Weinstein, S.L.1    Finn, A.J.2    Dave, S.H.3
  • 11
    • 0141780844 scopus 로고    scopus 로고
    • Stimulation of signal transducer and activator of transcription-1 (STAT1)-dependent gene transcription by lipopolysaccharide and interferon-g is regulated by mammalian target of rapamycin
    • Kristof AS, Marks-Konczalik J, Billings E et al. Stimulation of signal transducer and activator of transcription-1 (STAT1)-dependent gene transcription by lipopolysaccharide and interferon-g is regulated by mammalian target of rapamycin. J. Biol. Chem. 278, 33637-33644 (2003
    • (2003) J. Biol. Chem. , vol.278 , pp. 33637-33644
    • Kristof, A.S.1    Marks-Konczalik, J.2    Billings, E.3
  • 12
    • 33749522045 scopus 로고    scopus 로고
    • Rapamycin decreases leukocyte migration in vivo and effectively reduces experimentally induced chronic colitis
    • Farkas S, Hornung M, Sattler C et al. Rapamycin decreases leukocyte migration in vivo and effectively reduces experimentally induced chronic colitis. Int. J. Colorectal Dis. 21, 747-753 (2006
    • (2006) Int. J. Colorectal Dis. , vol.21 , pp. 747-753
    • Farkas, S.1    Hornung, M.2    Sattler, C.3
  • 13
    • 34247108064 scopus 로고    scopus 로고
    • Therapeutic effect of a new immunosuppressive agent, everolimus, on interleukin-10 gene-deficient mice with colitis
    • Matsuda C, Ito T, Song J et al. Therapeutic effect of a new immunosuppressive agent, everolimus, on interleukin-10 gene-deficient mice with colitis. Clin. Exp. Immunol. 148, 348-359 (2007
    • (2007) Clin. Exp. Immunol. , vol.148 , pp. 348-359
    • Matsuda, C.1    Ito, T.2    Song, J.3
  • 14
    • 65549160091 scopus 로고    scopus 로고
    • Synthesis and therapeutic evaluation of pyridyl based novel mTOR inhibitors
    • Deore V, Yewalkar N, Bhatia D et al. Synthesis and therapeutic evaluation of pyridyl based novel mTOR inhibitors. Bioorg. Med. Chem. Lett. 19, 2949-2952 (2009
    • (2009) Bioorg. Med. Chem. Lett. , vol.19 , pp. 2949-2952
    • Deore, V.1    Yewalkar, N.2    Bhatia, D.3
  • 15
    • 33646582664 scopus 로고    scopus 로고
    • Hypothalamic mTOR signaling regulates food intake
    • Cota D, Proulx K, Smith KA et al. Hypothalamic mTOR signaling regulates food intake. Science 312, 927-930 (2006
    • (2006) Science , vol.312 , pp. 927-930
    • Cota, D.1    Proulx, K.2    Smith, K.A.3
  • 16
    • 67650944993 scopus 로고    scopus 로고
    • Rapamycin fed late in life extends lifespan in genetically heterogeneous mice
    • Harrison DE, Strong R, Sharp ZD et al. Rapamycin fed late in life extends lifespan in genetically heterogeneous mice. Nature 460, 392-395 (2009
    • (2009) Nature , vol.460 , pp. 392-395
    • Harrison, D.E.1    Strong, R.2    Sharp, Z.D.3
  • 17
    • 67749122122 scopus 로고    scopus 로고
    • Targeting PI3K signalling in cancer: Opportunities, challenges and limitations
    • Engelman JA. Targeting PI3K signalling in cancer: opportunities, challenges and limitations. Nat. Rev. Cancer 9, 550-562 (2009
    • (2009) Nat. Rev. Cancer , vol.9 , pp. 550-562
    • Engelman, J.A.1
  • 18
    • 68249093818 scopus 로고    scopus 로고
    • Targeting the phosphoinositide 3-kinase pathway in cancer
    • Liu P, Cheng H, Roberts TM et al. Targeting the phosphoinositide 3-kinase pathway in cancer. Nat. Rev. Drug Discov. 8, 627-644 (2009
    • (2009) Nat. Rev. Drug Discov. , vol.8 , pp. 627-644
    • Liu, P.1    Cheng, H.2    Roberts, T.M.3
  • 19
    • 63749129788 scopus 로고    scopus 로고
    • PI3K and mTOR inhibitors: A new generation of targeted anticancer agents
    • Brachmann S, Fritsch C, Maira SM et al. PI3K and mTOR inhibitors: a new generation of targeted anticancer agents. Curr. Opin. Cell Biol. 21, 194-198 (2009
    • (2009) Curr. Opin. Cell Biol. , vol.21 , pp. 194-198
    • Brachmann, S.1    Fritsch, C.2    Maira, S.M.3
  • 20
    • 68149096799 scopus 로고    scopus 로고
    • The pharmacology of mTOR inhibition: The quest for effective cancer therapies reveals insight into the regulation and function of the mammalian target of rapamycin
    • Guertin DA, Sabatini, DM. The pharmacology of mTOR inhibition: the quest for effective cancer therapies reveals insight into the regulation and function of the mammalian target of rapamycin. Science Signaling 2 (67), 24 (2009
    • (2009) Science Signaling , vol.2 , Issue.67 , pp. 24
    • Guertin, D.A.1    Sabatini, D.M.2
  • 21
    • 70350418625 scopus 로고    scopus 로고
    • Sabatini DM. mTOR signaling at a glance
    • Laplante M, Sabatini DM. mTOR signaling at a glance. J. Cell Sci. 122, 3589-3594 (2009
    • (2009) J. Cell Sci. , vol.122 , pp. 3589-3594
    • Laplante, M.1
  • 23
    • 68049126433 scopus 로고    scopus 로고
    • Signaling events downstream of mammalian target of rapamycin complex 2 are attenuated in cells and tumors deficient for the tuberous sclerosis complex tumor suppressors
    • Huang J, Wu S, Wu CL et al. Signaling events downstream of mammalian target of rapamycin complex 2 are attenuated in cells and tumors deficient for the tuberous sclerosis complex tumor suppressors. Cancer Res. 69, 6107-6114 (2009
    • (2009) Cancer Res. , vol.69 , pp. 6107-6114
    • Huang, J.1    Wu, S.2    Wu, C.L.3
  • 24
    • 10244260355 scopus 로고    scopus 로고
    • Anderson Combination of the mTOR inhibitor rapamycin and CC-5013 has synergistic activity in multiple myeloma
    • Raje N, Kumar S, Hideshima T et al. Anderson Combination of the mTOR inhibitor rapamycin and CC-5013 has synergistic activity in multiple myeloma. Blood 104, 4188-4193 (2004
    • (2004) Blood , vol.104 , pp. 4188-4193
    • Raje, N.1    Kumar, S.2    Hideshima, T.3
  • 25
    • 18144399578 scopus 로고    scopus 로고
    • MTOR-targeted therapy of cancer with rapamycin derivatives
    • Vignot S, Faivre S, Aguirre D et al. mTOR-targeted therapy of cancer with rapamycin derivatives. Annal. Oncology 16, 525-537 (2005
    • (2005) Annal. Oncology , vol.16 , pp. 525-537
    • Vignot, S.1    Faivre, S.2    Aguirre, D.3
  • 26
    • 34548700597 scopus 로고    scopus 로고
    • Rapamycin: Something old, something new, sometimes borrowed and now renewed
    • Hartford CM, Ratain MJ. Rapamycin: something old, something new, sometimes borrowed and now renewed. Clin. Pharmacol. Ther. 82, 381-388 (2007
    • (2007) Clin. Pharmacol. Ther. , vol.82 , pp. 381-388
    • Hartford, C.M.1    Ratain, M.J.2
  • 27
    • 33646023695 scopus 로고    scopus 로고
    • Prolonged rapamycin treatment inhibits mTORC2 assembly and Akt/PKB
    • Sarbassov DD, Ali SM et al. Prolonged rapamycin treatment inhibits mTORC2 assembly and Akt/PKB. Mol. Cell 22, 159-168 (2006
    • (2006) Mol. Cell , vol.22 , pp. 159-168
    • Sarbassov, D.D.1    Ali, S.M.2
  • 28
    • 0029842109 scopus 로고    scopus 로고
    • Structure of the FKBP12-rapamycin complex interacting with the binding domain of human FRAP
    • Choi J, Chen J, Schreiber SL et al. Structure of the FKBP12-rapamycin complex interacting with the binding domain of human FRAP. Science 273, 239-342 (1996
    • (1996) Science , vol.273 , pp. 239-342
    • Choi, J.1    Chen, J.2    Schreiber, S.L.3
  • 29
    • 32044465506 scopus 로고    scopus 로고
    • TOR signaling in growth and metabolism
    • Wullschleger S, Loewith R, Hall MN. TOR signaling in growth and metabolism. Cell 124, 471-484 (2006
    • (2006) Cell , vol.124 , pp. 471-484
    • Wullschleger, S.1    Loewith, R.2    Hall, M.N.3
  • 30
    • 33750211376 scopus 로고    scopus 로고
    • Predicted mechanisms of resistance to mTOR inhibitors
    • Kurmasheva RT, Huang S, Houghton PJ. Predicted mechanisms of resistance to mTOR inhibitors. Br. J. Cancer 95, 955-960 (2006
    • (2006) Br. J. Cancer , vol.95 , pp. 955-960
    • Kurmasheva, R.T.1    Huang, S.2    Houghton, P.J.3
  • 31
    • 0346362997 scopus 로고    scopus 로고
    • Rapamycins: Mechanism of action and cellular resistance
    • Huang S, Bjornsti MA, Houghton PJ. Rapamycins: mechanism of action and cellular resistance. Cancer Biol. Ther. 2, 222-232 (2003
    • (2003) Cancer Biol. Ther. , vol.2 , pp. 222-232
    • Huang, S.1    Bjornsti, M.A.2    Houghton, P.J.3
  • 32
    • 0038339003 scopus 로고    scopus 로고
    • Phospholipase D confers rapamycin resistance in human breast cancer cells
    • Chen Y, Zheng Y et al. Phospholipase D confers rapamycin resistance in human breast cancer cells. Oncogene 22, 3937-3942 (2003
    • (2003) Oncogene , vol.22 , pp. 3937-3942
    • Chen, Y.1    Zheng, Y.2
  • 33
    • 0034969478 scopus 로고    scopus 로고
    • Langrehr JM. mTOR inhibitors: An overview
    • Neuhaus P, Klupp J, Langrehr JM. mTOR inhibitors: an overview. Liv. Transplantation 7, 473-484 (2001
    • (2001) Liv. Transplantation , vol.7 , pp. 473-484
    • Neuhaus, P.1    Klupp, J.2
  • 34
    • 0016713286 scopus 로고
    • Rapamycin (AY-22989), a new antifungal antibiotic. II. Fermentation, isolation and characterization
    • Tokyo
    • Sehgal SN, Baker H, Vezina C. Rapamycin (AY-22,989), a new antifungal antibiotic. II. Fermentation, isolation and characterization. J. Antibiot. (Tokyo) 28, 727-732 (1975
    • (1975) J. Antibiot , vol.28 , pp. 727-732
    • Sehgal, S.N.1    Baker, H.2    Vezina, C.3
  • 35
    • 0017362502 scopus 로고
    • Inhibition of the immune response by rapamycin, a new antifungal antibiotic
    • Martel RR, Klicius J, Galet S. Inhibition of the immune response by rapamycin, a new antifungal antibiotic. Can. J. Physiol. Pharmacol. 55, 48-51 (1977
    • (1977) Can. J. Physiol. Pharmacol. , vol.55 , pp. 48-51
    • Martel, R.R.1    Klicius, J.2    Galet, S.3
  • 36
    • 0032823635 scopus 로고    scopus 로고
    • Antifungal activities of antineoplastic agents: Saccharomyces cerevisiae as a model system to study drug action
    • Cardenas ME, Cruz MC, Del Poeta M et al. Antifungal activities of antineoplastic agents: Saccharomyces cerevisiae as a model system to study drug action. Clin. Microbiol. Rev. 12, 583-611 (1999
    • (1999) Clin. Microbiol. Rev. , vol.12 , pp. 583-611
    • Cardenas, M.E.1    Cruz, M.C.2    Del Poeta, M.3
  • 37
    • 1842473009 scopus 로고    scopus 로고
    • Antifungal attributes of immunosuppressive agents: New paradigms in management and elucidating the pathophysiologic basis of opportunistic mycoses in organ transplant recipients
    • Singh N, Heitman J. Antifungal attributes of immunosuppressive agents: new paradigms in management and elucidating the pathophysiologic basis of opportunistic mycoses in organ transplant recipients. Transplantation 77, 795-800 (2004
    • (2004) Transplantation , vol.77 , pp. 795-800
    • Singh, N.1    Heitman, J.2
  • 38
    • 15844391440 scopus 로고    scopus 로고
    • Mechanism of action of the immunosuppressant rapamycin
    • Dumont FJ, Su Q. Mechanism of action of the immunosuppressant rapamycin. Life Sci. 58, 373-395 (1996
    • (1996) Life Sci. , vol.58 , pp. 373-395
    • Dumont, F.J.1    Su, Q.2
  • 39
    • 38049187096 scopus 로고    scopus 로고
    • Mammalian target of rapamycin (mTOR) inhibition activates phosphatidylinositol 3-kinase/Akt by up-regulating insulin-like growth factor-1 receptor signaling in acute myeloid leukemia: Rationale for therapeutic inhibition of both pathways
    • Tamburini J, Chapuis N, Bardet V et al. Mammalian target of rapamycin (mTOR) inhibition activates phosphatidylinositol 3-kinase/Akt by up-regulating insulin-like growth factor-1 receptor signaling in acute myeloid leukemia: rationale for therapeutic inhibition of both pathways. Blood 111, 379-382 (2008
    • (2008) Blood , vol.111 , pp. 379-382
    • Tamburini, J.1    Chapuis, N.2    Bardet, V.3
  • 40
    • 70349576526 scopus 로고    scopus 로고
    • Protein synthesis is resistant to rapamycin and constitutes a promising therapeutic target in acute myeloid leukemia
    • Tamburini J, Green AS, Bardet V et al. Protein synthesis is resistant to rapamycin and constitutes a promising therapeutic target in acute myeloid leukemia. Blood 114, 1618-1627 (2009
    • (2009) Blood , vol.114 , pp. 1618-1627
    • Tamburini, J.1    Green, A.S.2    Bardet, V.3
  • 41
    • 70349199015 scopus 로고    scopus 로고
    • Identification and optimisation of novel and selective small molecular weight kinase inhibitors of mTOR
    • Menear KA, Gomez S, Malagu K et al. Identification and optimisation of novel and selective small molecular weight kinase inhibitors of mTOR. Bioorg. Med. Chem. Lett. 19, 5898-5901 (2009
    • (2009) Bioorg. Med. Chem. Lett. , vol.19 , pp. 5898-5901
    • Menear, K.A.1    Gomez, S.2    Malagu, K.3
  • 42
    • 77950050825 scopus 로고    scopus 로고
    • Triazines incorporating (R)-3-methylmorpholine are potent inhibitors of the mammalian target of rapamycin (mTOR) with selectivity over PI3Ka
    • Richard DJ, Verheijen JC, Yu K et al. Triazines incorporating (R)-3-methylmorpholine are potent inhibitors of the mammalian target of rapamycin (mTOR) with selectivity over PI3Ka. Bioorg. Med. Chem. Lett. 2010, 20, 2654-2657 (2010
    • (2010) Bioorg. Med. Chem. Lett. , vol.2010 , Issue.20 , pp. 2654-2657
    • Richard, D.J.1    Verheijen, J.C.2    Yu, K.3
  • 43
    • 70349256453 scopus 로고    scopus 로고
    • The discovery and optimization of pyrido[2,3-d] pyrimidine-2,4-diamines as potent and selective inhibitors of mTOR kinase
    • Malagu K, Duggan H, Menear K et al. The discovery and optimization of pyrido[2,3-d] pyrimidine-2,4-diamines as potent and selective inhibitors of mTOR kinase. Bioorg. Med. Chem. Lett. 19, 5950-5953 (2009
    • (2009) Bioorg. Med. Chem. Lett. , Issue.19 , pp. 5950-5953
    • Malagu, K.1    Duggan, H.2    Menear, K.3
  • 44
    • 67650312583 scopus 로고    scopus 로고
    • Ku-0063794 is a specific inhibitor of the mammalian target of rapamycin (mTOR
    • Garcia-Martinez JM, Moran J, Clarke RG et al. Ku-0063794 is a specific inhibitor of the mammalian target of rapamycin (mTOR). Biochem. J. 421, 29-42 (2009
    • (2009) Biochem. J. , vol.421 , pp. 29-42
    • Garcia-Martinez, J.M.1    Moran, J.2    Clarke, R.G.3
  • 45
    • 69049087738 scopus 로고    scopus 로고
    • ATP-competitive inhibitors of the mammalian target of rapamycin: Design and synthesis of highly potent and selective pyrazolopyrimidines
    • Zask A, Verheijen JC, Curran K et al. ATP-competitive inhibitors of the mammalian target of rapamycin: design and synthesis of highly potent and selective pyrazolopyrimidines. J. Med. Chem. 52, 5013-5016 (2009
    • (2009) J. Med. Chem. , vol.52 , pp. 5013-5016
    • Zask, A.1    Verheijen, J.C.2    Curran, K.3
  • 46
    • 73249140565 scopus 로고    scopus 로고
    • Morpholine derivatives greatly enhance the selectivity of mammalian target of rapamycin (mTOR) inhibitors
    • Zask A, Kaplan J, Verheijen JC et al. Morpholine derivatives greatly enhance the selectivity of mammalian target of rapamycin (mTOR) inhibitors. J. Med. Chem. 52, 7942-7945 (2009
    • (2009) J. Med. Chem. , vol.52 , pp. 7942-7945
    • Zask, A.1    Kaplan, J.2    Verheijen, J.C.3
  • 47
    • 71849089048 scopus 로고    scopus 로고
    • Incorporation of water-solubilizing groups in pyrazolopyrimidine mTOR inhibitors: Discovery of highly potent and selective analogs with improved human microsomal stability
    • Richard DJ, Verheijen JC, Curran K et al. Incorporation of water-solubilizing groups in pyrazolopyrimidine mTOR inhibitors: discovery of highly potent and selective analogs with improved human microsomal stability. Bioorg. Med. Chem. Lett. 19, 6830-6835 (2009
    • (2009) Bioorg. Med. Chem. Lett. , vol.19 , pp. 6830-6835
    • Richard, D.J.1    Verheijen, J.C.2    Curran, K.3
  • 48
    • 75449120554 scopus 로고    scopus 로고
    • Pyrazolopyrimidines as highly potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): Optimization of the 1-substituent
    • Curran KJ, Verheijen JC, Kaplan J et al. Pyrazolopyrimidines as highly potent and selective, ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): optimization of the 1-substituent. Bioorg. Med. Chem. Lett. 20, 1440-1444 (2010
    • (2010) Bioorg. Med. Chem. Lett. , vol.20 , pp. 1440-1444
    • Curran, K.J.1    Verheijen, J.C.2    Kaplan, J.3
  • 49
    • 77950031107 scopus 로고    scopus 로고
    • 2-arylureidophenyl-4-(3-oxa-8-azabicyclo[3.2.1]octan-8-yl)triazines as highly potent and selective ATP competitive mTOR inhibitors: Optimization of human microsomal stability
    • Verheijen JC, Richard DJ, Curran K et al. 2-arylureidophenyl-4-(3-oxa-8- azabicyclo[3.2.1]octan-8-yl)triazines as highly potent and selective ATP competitive mTOR inhibitors: optimization of human microsomal stability. Bioorg. Med. Chem. Lett. 20, 2648-2653 (2010
    • (2010) Bioorg. Med. Chem. Lett. , vol.20 , pp. 2648-2653
    • Verheijen, J.C.1    Richard, D.J.2    Curran, K.3
  • 50
    • 77950055909 scopus 로고    scopus 로고
    • Discovery of 2-ureidophenyltriazines bearing bridged morpholines as potent and selective ATP-competitive mTOR inhibitors
    • Zask A, Verheijen JC, Richard DJ et al. Discovery of 2- ureidophenyltriazines bearing bridged morpholines as potent and selective ATP-competitive mTOR inhibitors. Bioorg. Med. Chem. Lett. 20, 2644-2647 (2010
    • (2010) Bioorg. Med. Chem. Lett. , vol.20 , pp. 2644-2647
    • Zask, A.1    Verheijen, J.C.2    Richard, D.J.3
  • 51
    • 72049122106 scopus 로고    scopus 로고
    • Discovery of 2-arylthieno[3,2-d] pyrimidines containing 8-oxa-3-azabi-cyclo[3.2.1]octane in the 4-position as potent inhibitors of mTOR with selectivity over PI3K
    • Verheijen JC, Yu K, Toral-Barza L et al. Discovery of 2-arylthieno[3,2-d] pyrimidines containing 8-oxa-3-azabi-cyclo[3.2.1]octane in the 4-position as potent inhibitors of mTOR with selectivity over PI3K. Bioorg. Med. Chem. Lett. 20, 375-379 (2010
    • (2010) Bioorg. Med. Chem. Lett. , vol.20 , pp. 375-379
    • Verheijen, J.C.1    Yu, K.2    Toral-Barza, L.3
  • 52
    • 77249098372 scopus 로고    scopus 로고
    • Lead optimization of N-3-substituted 7-morpholinotriazolopyrimidines as dual phosphoinositide 3-kinase/mammalian target of rapamycin inhibitors: Discovery of PKI-402
    • Dehnhardt CM, Venkatesan AM, Santos ED et al. Lead optimization of N-3-substituted 7-morpholinotriazolopyrimidines as dual phosphoinositide 3-kinase/mammalian target of rapamycin inhibitors: discovery of PKI-402. J. Med. Chem. 53 (2), 798-810 (2010
    • (2010) J. Med. Chem. , vol.53 , Issue.2 , pp. 798-810
    • Dehnhardt, C.M.1    Venkatesan, A.M.2    Santos, E.D.3
  • 53
    • 72249111293 scopus 로고    scopus 로고
    • Novel imidazolopyrimidines as dual PI3-kinase/mTOR inhibitors
    • Venkatesan AM, Dehnhardt CM, Chen Z et al. Novel imidazolopyrimidines as dual PI3-kinase/mTOR inhibitors. Bioorg. Med. Chem. Lett. 20, 653-656 (2010
    • (2010) Bioorg. Med. Chem. Lett. , vol.20 , pp. 653-656
    • Venkatesan, A.M.1    Dehnhardt, C.M.2    Chen, Z.3
  • 54
    • 77949492415 scopus 로고    scopus 로고
    • Discovery and optimization of 2-(4-substituted-pyrrolo[2,3-b]pyridin-3- yl) methylene-4-hydroxybenzofuran-3(2H)-ones as potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR)
    • Tsou HR, MacEwan G, Birnberg G et al. Discovery and optimization of 2-(4-substituted-pyrrolo[2,3-b]pyridin-3-yl) methylene-4-hydroxybenzofuran-3(2H) -ones as potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR). Bioorg. Med. Chem. Lett. 20, 2321-2325 (2010
    • (2010) Bioorg. Med. Chem. Lett. , vol.20 , pp. 2321-2325
    • Tsou, H.R.1    MacEwan, G.2    Birnberg, G.3
  • 55
    • 72249090391 scopus 로고    scopus 로고
    • Discovery of 3 6-dihydro-2H-pyran as a morpholine replacement in 6-aryl-1H-pyrazolo[3,4-d]pyrimidines and 2-arylthieno[3,2-d]pyrimidines: ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR)
    • Kaplan J, Verheijen JC, Brooijmans N et al. Discovery of 3,6-dihydro-2H-pyran as a morpholine replacement in 6-aryl-1H-pyrazolo[3,4-d] pyrimidines and 2-arylthieno[3,2-d]pyrimidines: ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR). Bioorg. Med. Chem. Lett. 20, 640-643 (2010
    • (2010) Bioorg. Med. Chem. Lett. , vol.20 , pp. 640-643
    • Kaplan, J.1    Verheijen, J.C.2    Brooijmans, N.3
  • 56
    • 77954638677 scopus 로고    scopus 로고
    • Discovery of GSK2126458, a highly potent inhibitor of PI3K and the mammalian target of rapapmycin
    • Knight SD, Adams ND, Burgess JL et al. Discovery of GSK2126458, a highly potent inhibitor of PI3K and the mammalian target of rapapmycin. ACS Med. Chem. Lett. 1(1), 39-43 (2010
    • (2010) ACS Med. Chem. Lett. , vol.1 , Issue.1 , pp. 39-43
    • Knight, S.D.1    Adams, N.D.2    Burgess, J.L.3
  • 57
    • 67651155960 scopus 로고    scopus 로고
    • Biological properties of potent inhibitors of class i phosphatidylinositide 3-kinases: From PI-103 through PI-540. PI-620 to the oral agent GDC-0941
    • Raynaud FI, Eccles SA, Patel S et al. Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: from PI-103 through PI-540, PI-620 to the oral agent GDC-0941. Mol. Cancer Ther. 8(7), 1725-1738 (2009
    • (2009) Mol. Cancer Ther. , vol.8 , Issue.7 , pp. 1725-1738
    • Raynaud, F.I.1    Eccles, S.A.2    Patel, S.3
  • 58
    • 58149509984 scopus 로고    scopus 로고
    • Take your PIK: Phosphatidylinositol 3-kinase inhibitors race through the clinic and toward cancer therapy
    • Ihle NT, Powis G. Take your PIK: phosphatidylinositol 3-kinase inhibitors race through the clinic and toward cancer therapy. Mol. Cancer Ther. 8(1), 1-9 (2009
    • (2009) Mol. Cancer Ther. , vol.8 , Issue.1 , pp. 1-9
    • Ihle, N.T.1    Powis, G.2
  • 59
    • 38149120449 scopus 로고    scopus 로고
    • Targeting phosphoinositide 3-kinase-moving towards therapy
    • Marone R, Cmiljanovic V, Giese B et al. Targeting phosphoinositide 3-kinase-moving towards therapy. Biochim. Biophys. Acta. 1784, 159-185 (2008
    • (2008) Biochim. Biophys. Acta. , vol.1784 , pp. 159-185
    • Marone, R.1    Cmiljanovic, V.2    Giese, B.3
  • 60
    • 59749099026 scopus 로고    scopus 로고
    • PI3K inhibitors for cancer treatment: Where do we stand?
    • Maira SM, Stauffer F, Schnell C et al. PI3K inhibitors for cancer treatment: where do we stand? Biochem Soc. Trans. 37, 265-272 (2009
    • (2009) Biochem Soc Trans. , vol.37 , pp. 265-272
    • Maira, S.M.1    Stauffer, F.2    Schnell, C.3
  • 61
    • 77953439691 scopus 로고    scopus 로고
    • Discovery of novel anticancer therapeutics targeting the PI3K/AKt/mTOR pathway
    • Maira SM, Furet P, Stauffer F. Discovery of novel anticancer therapeutics targeting the PI3K/AKt/mTOR pathway. Future Med. Chem. 1(1), 137-155 (2009
    • (2009) Future Med. Chem. , vol.1 , Issue.1 , pp. 137-155
    • Maira, S.M.1    Furet, P.2    Stauffer, F.3


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.