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Volumn 20, Issue 14, 2010, Pages 4228-4232

Synthesis and biological evaluation of 2-pyridyl-substituted pyrazoles and imidazoles as transforming growth factor-β type 1 receptor kinase inhibitors

Author keywords

ALK5 inhibitor; Cell based luciferase reporter assays; TGF

Indexed keywords

3 (3 (6 METHYLPYRIDIN 2 YL) 4 (QUINOLIN 6 YL) 1H PYRAZOLE 1 CARBOTHIOAMIDO)BENZAMIDE; 4 [4 (1,3 BENZODIOXOL 5 YL) 5 (2 PYRIDINYL) 1H IMIDAZOL 2 YL]BENZAMIDE; IMIDAZOLE DERIVATIVE; PROTEIN TYROSINE KINASE INHIBITOR; PYRAZOLE DERIVATIVE; SB 505124; SB 525334; TRANSFORMING GROWTH FACTOR BETA RECEPTOR 1; UNCLASSIFIED DRUG;

EID: 77953873137     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.05.032     Document Type: Article
Times cited : (32)

References (40)
  • 35
    • 77953872506 scopus 로고    scopus 로고
    • Blumberg, L. C.; Munchhof, M. J. World Patent WO 04/026863, 2004, p 72.
    • Blumberg, L. C.; Munchhof, M. J. World Patent WO 04/026863, 2004, p 72.
  • 36
    • 77953870078 scopus 로고    scopus 로고
    • Blumberg, L. C.; Munchhof, M. J.; Shavnya, A. U.S. Pat. Appl. Publ. US 2004/0176390, 2004, p 35.
    • Blumberg, L. C.; Munchhof, M. J.; Shavnya, A. U.S. Pat. Appl. Publ. US 2004/0176390, 2004, p 35.
  • 37
    • 77953871051 scopus 로고    scopus 로고
    • note
    • 4 in 24-well plates. The next day, when they reach approximately 90% confluence, cells were transfected with 0.1 μg of p3TP-Luc reporter construct, ARE-Luc reporter construct, or SBE-Luc reporter construct and 0.1 μg of β-galactosidase, using Lipofectamine 2000 (Invitrogen). At 24 h after transfection, various concentrations of ALK5 inhibitors were added to the cells. After 2 h, cells were treated with 5 ng/mL of TGF-β for 18-24 h. Cell lysates were harvested according to the manufacturer's instruction, and luminescence was measured by a luminometer VICTOR (Perkin-Elmer Life).


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.