2. Academic Validation
  3. 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

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

  • Bioorg Med Chem. 2011 Apr 15;19(8):2633-40. doi: 10.1016/j.bmc.2011.03.008.
Cheng Hua Jin 1,  Maddeboina Krishnaiah,  Domalapally Sreenu,  Kota Sudhakar Rao,  Vura Bala Subrahmanyam,  Chul-Yong Park,  Jee-Yeon Son,  Yhun Yhong Sheen,  Dae-Kee Kim
Affiliations

Affiliation

  • 1 College of Pharmacy, Ewha Womans University, Seoul, Republic of Korea.
PMID: 21435890 DOI: 10.1016/j.bmc.2011.03.008
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.

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