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.

Cheng Hua Jin,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

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.

2012

Cheng Hua Jin
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

Title compound (VIIb), the most potent derivative synthesized, inhibits ALK5 phosphorylation with an IC50 value of 0.57 nM and shows 94% inhibition at 100 nM in a luciferase reporter assay.

Keywords:

Luciferase
Stereochemistry
IC50
Phosphorylation
Kinase
Reporter gene
Receptor
Chemistry
Organic chemistry
Transforming growth factor
biological evaluation
triazole derivatives
luciferase reporter

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