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Synthesis and biological evaluation of 1-substituted-3(5)-(6-methylpyridin- 2-yl)-4-(quinolin-6-yl)pyrazoles as transforming growth factor-β type 1 receptor kinase inhibitors

Title: Synthesis and biological evaluation of 1-substituted-3(5)-(6-methylpyridin- 2-yl)-4-(quinolin-6-yl)pyrazoles as transforming growth factor-β type 1 receptor kinase inhibitors

Authors: Jin C.H.; Krishnaiah M.; Sreenu D.; Rao K.S.; Subrahmanyam V.B.; Park C.-Y.; Son J.-Y.; Sheen Y.Y.; Kim D.-K.

Ewha Authors: 신윤용; 김대기

SCOPUS Author ID: 신윤용; 김대기

Issue Date: 2011

Journal Title: Bioorganic and Medicinal Chemistry

ISSN: 0968-0896

Citation: Bioorganic and Medicinal Chemistry vol. 19, no. 8, pp. 2633 - 2640

Indexed: SCI; SCIE; SCOPUS

Document Type: Article

Abstract: A series of 1-substituted-3(5)-(6-methylpyridin-2-yl)-4-(quinolin-6-yl) pyrazoles 14a-e, 15a-e, 17a-c, and 18a-d have been synthesized and evaluated for their ALK5 inhibitory activity in an enzyme assay and in a cell-based luciferase reporter assay. The 6-quinolinyl pyrazole analogue 14b inhibited ALK5 phosphorylation with IC 50 value of 0.022 μM and showed 84% inhibition at 0.1 μM in a luciferase reporter assay using HaCaT cells permanently transfected with p3TP-luc reporter construct. © 2011 Elsevier Ltd. All rights reserved.