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

Purushottam M. Dewang; Dae Kee Kim

doi:10.1016/j.bmcl.2010.05.032

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

Purushottam M. Dewang, Dae Kee Kim

Department of Pharmaceutical Sciences

Research output: Contribution to journal › Article › peer-review

32 Scopus citations

Abstract

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.

Original language	English
Pages (from-to)	4228-4232
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	20
Issue number	14
DOIs	https://doi.org/10.1016/j.bmcl.2010.05.032
State	Published - 15 Jul 2010

Bibliographical note

Funding Information:
This work was supported by a grant from Ministry of Commerce, Industry and Energy, Korea ( 10027900 ).

Keywords

ALK5 inhibitor
Cell-based luciferase reporter assays
TGF-β

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10.1016/j.bmcl.2010.05.032

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

abstract = "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.",

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AU - Kim, Dae Kee

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

Abstract

Bibliographical note

Keywords

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