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Synthesis and biological evaluation of 2-benzylamino-4(5)-(6-methylpyridin- 2-yl)-5(4)-([1,2,4]triazolo[1,5-a]-pyridin-6-yl)thiazoles as transforming growth factor-β type 1 receptor kinase inhibitors

Title: Synthesis and biological evaluation of 2-benzylamino-4(5)-(6-methylpyridin- 2-yl)-5(4)-([1,2,4]triazolo[1,5-a]-pyridin-6-yl)thiazoles as transforming growth factor-β type 1 receptor kinase inhibitors

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

Ewha Authors: 신윤용; 김대기; 김승원

SCOPUS Author ID: 신윤용; 김대기; 김승원

Issue Date: 2012

Journal Title: European Journal of Medicinal Chemistry

ISSN: 0223-5234

Citation: European Journal of Medicinal Chemistry vol. 57, pp. 74 - 84

Indexed: SCI; SCIE; SCOPUS

Document Type: Article

Abstract: A series of 2-benzylamino-4(5)-(6-methylpyridin-2-yl)-5(4)-([1,2,4] triazolo[1,5-a]pyridin-6-yl)thiazoles 12a-ab, 13a, 13b, and 18a-d has been synthesized and evaluated for their ALK5 inhibitory activity in an enzyme assay and in a cell-based luciferase reporter assay. The N-(3-fluorobenzyl)-4-(6- methylpyridin-2-yl)-5-([1,2,4]triazolo[1,5-a]pyridin-6-yl)thiazol-2-amine (12b) inhibited ALK5 phosphorylation with an IC50 value of 7.01 nM and showed 61% inhibition at 30 nM in a luciferase reporter assay using HaCaT cells permanently transfected with p3TP-luc reporter construct. © 2012 Elsevier Masson SAS. All rights reserved.