Discovery of pyrazolo[1,5-a]pyridines as p110α-selective PI3 kinase inhibitors

Add time:08/04/2019    Source:sciencedirect.com

We have made a novel series of pyrazolo[1,5-a]pyridines as PI3 kinase inhibitors, and demonstrated their selectivity for the p110α isoform over the other Class Ia PI3 kinases. We investigated the SAR around the pyrazolo[1,5-a]pyridine ring system, and found compound 5x to be a particularly potent example (p110α IC50 0.9 nM). This compound inhibits cell proliferation and phosphorylation of Akt/PKB, a downstream marker of PI3 kinase activity, and showed in vivo activity in an HCT-116 human xenograft model.

We also recommend Trading Suppliers and Manufacturers of 3-Iodopyrazolo[1,5-a]pyridine, 97% (cas 19363-99-6). Pls Click Website Link as below: cas 19363-99-6 suppliers

Prev:Discovery and SAR of novel pyrazolo[1,5-a]pyrimidines as inhibitors of CDK9
Next:Enantioselective synthesis of 3-hydroxypiperidin-2-one (cas 19365-08-3)s)