2. Academic Validation
  3. 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

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

  • Eur J Med Chem. 2012 Nov:57:74-84. doi: 10.1016/j.ejmech.2012.09.011.
Maddeboina Krishnaiah 1,  Cheng Hua Jin,  Domalapally Sreenu,  Vura Bala Subrahmanyam,  Kota Sudhakar Rao,  Do-Hyun Son,  Hyun-Ju Park,  Seung Won Kim,  Yhun Yhong Sheen,  Dae-Kee Kim
Affiliations

Affiliation

  • 1 College of Pharmacy, Ewha Womans University, 11-1 Daehyun-dong, Seodaemun-gu, Seoul 120-750, South Korea.
PMID: 23047226 DOI: 10.1016/j.ejmech.2012.09.011
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 IC(50) 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.

Figures
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