2. Academic Validation
  3. Synthesis and biological evaluation of 1-substituted-3-(6-methylpyridin-2-yl)-4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)pyrazoles as transforming growth factor-β type 1 receptor kinase inhibitors

Synthesis and biological evaluation of 1-substituted-3-(6-methylpyridin-2-yl)-4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)pyrazoles as transforming growth factor-β type 1 receptor kinase inhibitors

  • Bioorg Med Chem Lett. 2011 Oct 15;21(20):6049-53. doi: 10.1016/j.bmcl.2011.08.064.
Cheng Hua Jin 1,  Maddeboina Krishnaiah,  Domalapally Sreenu,  Vura Bala Subrahmanyam,  Kota Sudhakar Rao,  Annaji Venkata Nagendra Mohan,  Chul-Yong Park,  Jee-Yeon Son,  Yhun Yhong Sheen,  Dae-Kee Kim
Affiliations

Affiliation

  • 1 College of Pharmacy, Ewha Womans University, 11-1 Daehyun-dong, Seodaemun-gu, Seoul 120-750, Republic of Korea.
PMID: 21911290 DOI: 10.1016/j.bmcl.2011.08.064
Abstract

A series of 1-substituted-3-(6-methylpyridin-2-yl)-4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)pyrazoles 14a-ae, 16a, 16b, and 21a-c has been prepared and evaluated for their ALK5 inhibitory activity in an Enzyme assay and in a cell-based luciferase reporter assay. The 4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-N-(4-methoxyphenyl)-3-(6-methylpyridin-2-yl)-1H-pyrazole-1-carbothioamide (14n) inhibited ALK5 phosphorylation with IC(50) value of 0.57 nM and showed 94% inhibition at 100 nM in a luciferase reporter assay using HaCaT cells permanently transfected with p3TP-luc reporter construct.

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