Add time:07/11/2019         Source:sciencedirect.com

3-{1-[(4-Fluorophenyl)sulfonyl]-1H-pyrazol-3-yl}-2-methylimidazo[1,2-a]pyridine, 2a, was discovered in our chemical library as a novel p110α inhibitor with an IC50 of 0.67 μM, through screening in a scintillation proximity assay. Optimization of the substituents of 2a increased the p110α inhibitory activity by more than 300-fold (2g: IC50 = 0.0018 μM). Further structural modification of 2g afforded thiazole derivative 12, which has potent p110α inhibitory activity (IC50 of 0.0028 μM) and is highly selective for p110α over other PI3K isoforms. Compound 12 also inhibited serum-induced cell proliferation of A375 and HeLa cells in vitro with IC50 values of 0.14 μM and 0.21 μM, respectively, and suppressed tumor growth by 37% in a mouse HeLa xenograft model when dosed intraperitoneally at 25 mg/kg. These results suggest that selective p110α inhibitors may have potential as cancer therapeutic agents.

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