TY - JOUR
T1 - Synthesis and biological evaluation of 2-pyridyl-substituted pyrazoles and imidazoles as transforming growth factor-β type 1 receptor kinase inhibitors
AU - Dewang, Purushottam M.
AU - Kim, Dae Kee
N1 - Funding Information:
This work was supported by a grant from Ministry of Commerce, Industry and Energy, Korea ( 10027900 ).
PY - 2010/7/15
Y1 - 2010/7/15
N2 - A series of 2-pyridyl-substituted pyrazoles (16a-d, 17, 18, and 28a-e) and imidazoles (22 and 23) has been synthesized and evaluated for their ALK5 inhibitory activity in cell-based luciferase reporter assays. Among them, 3-(3-(6-methylpyridin-2-yl)-4-(quinolin-6-yl)-1H-pyrazole-1-carbothioamido)benzamide (28c) showed 96% and 93% inhibition at 0.1 μM in luciferase reporter assays using HaCaT cells transiently transfected with p3TP-luc reporter construct and ARE-luc reporter construct, respectively.
AB - A series of 2-pyridyl-substituted pyrazoles (16a-d, 17, 18, and 28a-e) and imidazoles (22 and 23) has been synthesized and evaluated for their ALK5 inhibitory activity in cell-based luciferase reporter assays. Among them, 3-(3-(6-methylpyridin-2-yl)-4-(quinolin-6-yl)-1H-pyrazole-1-carbothioamido)benzamide (28c) showed 96% and 93% inhibition at 0.1 μM in luciferase reporter assays using HaCaT cells transiently transfected with p3TP-luc reporter construct and ARE-luc reporter construct, respectively.
KW - ALK5 inhibitor
KW - Cell-based luciferase reporter assays
KW - TGF-β
UR - http://www.scopus.com/inward/record.url?scp=77953873137&partnerID=8YFLogxK
U2 - 10.1016/j.bmcl.2010.05.032
DO - 10.1016/j.bmcl.2010.05.032
M3 - Article
C2 - 20621731
AN - SCOPUS:77953873137
SN - 0960-894X
VL - 20
SP - 4228
EP - 4232
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
IS - 14
ER -