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

Browse

My Repository

View : 572 Download: 0

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

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

Ewha Authors: 신윤용; 김대기

SCOPUS Author ID: 신윤용; 김대기

Issue Date: 2011

Journal Title: European Journal of Medicinal Chemistry

ISSN: 0223-5234

Citation: European Journal of Medicinal Chemistry vol. 46, no. 9, pp. 3917 - 3925

Indexed: SCI; SCIE; SCOPUS

Document Type: Article

Abstract: A series of 1-substituted-3(5)-(6-methylpyridin-2-yl)-4-(quinoxalin-6-yl) pyrazoles 14a-d, 15a-d, 17a, 17b, 18a-d, 19a, and 19b has been synthesized and evaluated for their ALK5 inhibitory activity in an enzyme assay and in a cell-based luciferase reporter assay. The 2-[3-(6-methylpyridin-2-yl)-4- (quinoxalin-6-yl)-1H-pyrazol-1-yl]-N-phenylethanethioamide (18a) inhibited ALK5 phosphorylation with an IC 50 value of 0.013 μM and showed 80% inhibition at 0.1 μM in a luciferase reporter assay using HaCaT cells permanently transfected with p3TP-luc reporter construct. © 2011 Elsevier Masson SAS. All rights reserved.