메뉴 건너뛰기




Volumn 46, Issue 19, 2003, Pages 3953-3956

Synthesis and activity of new aryl- and heteroaryl-substituted pyrazole inhibitors of the transforming growth factor-β type I receptor kinase domain

Author keywords

[No Author keywords available]

Indexed keywords

4 (QUINOLIN 4 YL)PYRAZOLE DERIVATIVE; MITOGEN ACTIVATED PROTEIN KINASE; POLYCYCLIC AROMATIC HYDROCARBON DERIVATIVE; PROTEIN TYROSINE KINASE; PROTEIN TYROSINE KINASE INHIBITOR; PYRAZOLE DERIVATIVE; TRANSFORMING GROWTH FACTOR BETA RECEPTOR; UNCLASSIFIED DRUG;

EID: 0037620888     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm0205705     Document Type: Article
Times cited : (222)

References (23)
  • 1
    • 0034796457 scopus 로고    scopus 로고
    • The TGFβ receptor activation process: An inhibitor- to substrate-binding switch
    • (a) Huse, M.; Muir, R. W.; Xu, L.; Chen, Y.-G.; Kuriyan, J.; Massague, J. The TGFβ Receptor Activation Process: An Inhibitor- to Substrate-Binding Switch. Mol. Cell 2001, 8, 671-682.
    • (2001) Mol. Cell , vol.8 , pp. 671-682
    • Huse, M.1    Muir, R.W.2    Xu, L.3    Chen, Y.-G.4    Kuriyan, J.5    Massague, J.6
  • 2
    • 0035694910 scopus 로고    scopus 로고
    • Smad regulation in TGF-β signal transduction
    • (b) Moustakas, A.; Soucheinytskyi, S.; Heldin, C.-H. Smad Regulation in TGF-β Signal Transduction. J. Cell Sci. 2001, 114, 4359-4369.
    • (2001) J. Cell Sci. , vol.114 , pp. 4359-4369
    • Moustakas, A.1    Soucheinytskyi, S.2    Heldin, C.-H.3
  • 3
    • 0034673972 scopus 로고    scopus 로고
    • Transforming growth factor β signaling mediators
    • (c) Zimmerman, C. M.; Padgett, R. W. Transforming Growth Factor β Signaling Mediators and Modulators. Gene 2000, 249, 17-30.
    • (2000) Modulators. Gene , vol.249 , pp. 17-30
    • Zimmerman, C.M.1    Padgett, R.W.2
  • 4
    • 0026708669 scopus 로고
    • Post-transcriptional regulation of the human transforming growth factor-β1 gene
    • Kim, S. J.; Park, K.; Koeller, D.; Kim, K. Y.; Wakefield, L. M.; Sporn, M. B.; Roberts, A. B. Post-transcriptional Regulation of the Human Transforming Growth Factor-β1 Gene. J. Biol. Chem. 1992, 267 (19), 13702-13707.
    • (1992) J. Biol. Chem. , vol.267 , Issue.19 , pp. 13702-13707
    • Kim, S.J.1    Park, K.2    Koeller, D.3    Kim, K.Y.4    Wakefield, L.M.5    Sporn, M.B.6    Roberts, A.B.7
  • 5
    • 0036127649 scopus 로고    scopus 로고
    • Beyond mitomycin: TGF-β and wound healing
    • Cordeiro, M. F. Beyond Mitomycin: TGF-β and Wound Healing. Prog. Retinal Eye Res. 2002, 21, 75-89.
    • (2002) Prog. Retinal Eye Res. , vol.21 , pp. 75-89
    • Cordeiro, M.F.1
  • 6
    • 0034802221 scopus 로고    scopus 로고
    • Functional role of TGFβ in Alzheimer's disease microvascular injury lessons from transgenic mice
    • Masliah, E.; Ho, G.; Wyss-Coray, T. Functional Role of TGFβ in Alzheimer's Disease Microvascular Injury: Lessons from Transgenic Mice. Neurochem. Int. 2001, 39, 393-400.
    • (2001) Neurochem. Int. , vol.39 , pp. 393-400
    • Masliah, E.1    Ho, G.2    Wyss-Coray, T.3
  • 7
    • 0033622125 scopus 로고    scopus 로고
    • TGF-βs and TGF-β receptors in atherosclerosis
    • McCaffrey, T. A. TGF-βs and TGF-β Receptors in Atherosclerosis. Cytokine Growth Factor Rev. 2000, 11, 103-114.
    • (2000) Cytokine Growth Factor Rev. , vol.11 , pp. 103-114
    • McCaffrey, T.A.1
  • 9
    • 0035724807 scopus 로고    scopus 로고
    • Transforming growth factor-β: Promising Target for anti-stenosis therapy
    • Chamberlain, J. Transforming Growth Factor-β: A Promising Target for Anti-Stenosis Therapy. Cardiovasc. Drug Rev. 2001, 19 (4), 329-344.
    • (2001) Cardiovasc. Drug Rev. , vol.19 , Issue.4 , pp. 329-344
    • Chamberlain, J.1
  • 10
    • 0035501062 scopus 로고    scopus 로고
    • TGF-β signaling in cancer - A double-edged sword
    • (a) Akhurst, R. J.; Derynk, R. TGF-β Signaling in Cancer - A Double-Edged Sword. Trends Cell Biol. 2001, 11 (11), S44-S51.
    • (2001) Trends Cell Biol. , vol.11 , Issue.11
    • Akhurst, R.J.1    Derynk, R.2
  • 11
    • 0034785348 scopus 로고    scopus 로고
    • TGF-β signaling in tumor suppression and cancer progression
    • (b) Derynk, R.; Akhurst, R. J.; Balmain, A. TGF-β Signaling in Tumor Suppression and Cancer Progression. Nat. Genet. 2001, 29, 117-129.
    • (2001) Nat. Genet. , vol.29 , pp. 117-129
    • Derynk, R.1    Akhurst, R.J.2    Balmain, A.3
  • 12
    • 0034644472 scopus 로고    scopus 로고
    • TGF-β signaling in growth control cancer, and heritable disorders
    • (c) Massague, J.; Blain, S. W.; Lo, R. S. TGF-β Signaling in Growth Control, Cancer, and Heritable Disorders. Cell 2000, 103, 295-309.
    • (2000) Cell , vol.103 , pp. 295-309
    • Massague, J.1    Blain, S.W.2    Lo, R.S.3
  • 13
    • 0034612789 scopus 로고    scopus 로고
    • Role of transforming growth factor-β signaling in cancer
    • (d) de Caestecker, M. P.; Piek, E.; Roberts, A. B. Role of Transforming Growth Factor-β Signaling in Cancer. J. Natl. Cancer Inst. 2000, 92 (17), 1388-1402.
    • (2000) J. Natl. Cancer Inst. , vol.92 , Issue.17 , pp. 1388-1402
    • De Caestecker, M.P.1    Piek, E.2    Roberts, A.B.3
  • 14
    • 0029022221 scopus 로고
    • GS domain mutations that constitutively activate Tβr-1, the downstream signaling component in the TGF-β receptor complex
    • Wieser, R.; Wrana, J. L.; Massague, J. GS Domain Mutations That Constitutively Activate TβR-1, the Downstream Signaling Component in the TGF-β Receptor Complex. EMBO J. 1995, 14 (10), 2199-2208.
    • (1995) EMBO J. , vol.14 , Issue.10 , pp. 2199-2208
    • Wieser, R.1    Wrana, J.L.2    Massague, J.3
  • 16
    • 0038641688 scopus 로고
    • Induction of c-sis mRNA and activity similar to platelet-derived growth factor by transforming growth factor beta: A proposed model for indirect Mitogenesis involving autocrine activity
    • Leof, E. B.; Proper, J. A.; Goustin, A. S.; Shipley, G. D.; DiCorleto, P. E.; Moses, H. L. Induction of c-sis mRNA and Activity Similar to Platelet-Derived Growth Factor by Transforming Growth Factor Beta: A Proposed Model for Indirect Mitogenesis Involving Autocrine Activity. Proc. Natl. Acad. Sci. U.S.A. 1986, 83 (8), 2453-2457.
    • (1986) Proc. Natl. Acad. Sci. U.S.A. , vol.83 , Issue.8 , pp. 2453-2457
    • Leof, E.B.1    Proper, J.A.2    Goustin, A.S.3    Shipley, G.D.4    DiCorleto, P.E.5    Moses, H.L.6
  • 19
    • 0032862832 scopus 로고    scopus 로고
    • Inhibitors of p38 map kinase: Therapeutic intervention in cytokine-mediated diseases
    • (c) Salituro, F. G.; Germann, U. A.; Wilson, K. P.; Bemis, G. W.; Fox, T.; Su, S.-S. Inhibitors of p38 MAP Kinase: Therapeutic Intervention in Cytokine-Mediated Diseases. Curr. Med. Chem. 1999, 6, 807-823.
    • (1999) Curr. Med. Chem. , vol.6 , pp. 807-823
    • Salituro, F.G.1    Germann, U.A.2    Wilson, K.P.3    Bemis, G.W.4    Fox, T.5    Su, S.-S.6
  • 20
    • 0037186459 scopus 로고    scopus 로고
    • Identification of novel inhibitors of the transforming growth factor β1 (TGF-β1) type I receptor (ALK5)
    • This 4-fluorophenyl/pyridin-2-yl substitution pattern has been employed recently in two different scaffolds developed for the selective inhibition of the TGF-β1 receptor kinase domain. (a) Callahan, J. F.; Burgess, J. L.; Fornwald, J. A.; Gaster, L. M.; Harling, J. D.; Harrington, F. P.; Heer, J.; Kwon, C.; Lehr, R.; Mather, A.; Olson, B. A.; Weinstock, J.; Laping, N. J. Identification of Novel Inhibitors of the Transforming Growth Factor β1 (TGF-β1) Type I Receptor (ALK5). J. Med. Chem. 2002, 45, 999-1001.
    • (2002) J. Med. Chem. , vol.45 , pp. 999-1001
    • Callahan, J.F.1    Burgess, J.L.2    Fornwald, J.A.3    Gaster, L.M.4    Harling, J.D.5    Harrington, F.P.6    Heer, J.7    Kwon, C.8    Lehr, R.9    Mather, A.10    Olson, B.A.11    Weinstock, J.12    Laping, N.J.13
  • 22
    • 0036085920 scopus 로고    scopus 로고
    • SB-431542 is a potent and specific inhibitor of transforming growth factor-β superfamily type I. Activin receptor-like kinase (ALK) receptors ALK4, ALK5, ALK7
    • (c) Inman, G. J.; Nicolas, F. J.; Callahan, J. F.; Harling, J. D.; Gaster, L. M.; Reith, A. D.; Laping, N. J.; Hill, C. S. SB-431542 Is a Potent and Specific Inhibitor of Transforming Growth Factor-β Superfamily Type I Activin Receptor-Like Kinase (ALK) Receptors ALK4, ALK5, and ALK7. Mol. Pharmacol. 2002, 62 (1), 65-74.
    • (2002) Mol. Pharmacol. , vol.62 , Issue.1 , pp. 65-74
    • Inman, G.J.1    Nicolas, F.J.2    Callahan, J.F.3    Harling, J.D.4    Gaster, L.M.5    Reith, A.D.6    Laping, N.J.7    Hill, C.S.8


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.