Synthesis and antitumor activity evaluation of PI3K inhibitors containing 3-substituted quinazolin-4(3H)-one moiety

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

In present study, a series of N-(2-methoxy-5-(3-substituted quinazolin-4(3H)-one-6-yl)-pyridin-3-yl)phenylsulfonamide were synthesized. Their antiproliferative activities in vitro were evaluated via MTT assay against HCT116 and MCF-7 cancer cell lines. The SAR of title compounds was discussed. The compounds (S)-C5 and (S)-C8 displayed potent inhibitory activity against PI3Ks and mTOR, especially against PI3Kα. In addition, compound (S)-C5 can efficaciously inhibit tumor growth in a mice S-180 model. These findings suggest that our designed compounds can serve as potent PI3K inhibitors and effective anticancer agents.

We also recommend Trading Suppliers and Manufacturers of 2-BroMo-1-(5-Methoxy-pyridin-3-yl)-ethanone (cas 1196145-15-9). Pls Click Website Link as below: cas 1196145-15-9 suppliers

Prev:1, 2-Dichloro-3,3-dimethylcyclopropene as a source of 1,2-dichlo-3-methylbut-2-enzylidene at ambient temperature
Next:Reaction of 5-(1-bromo-2-aryl-vinyl)-3-methyl-4-nitro-isoxazoles and 1,3-dicarbonyl compounds)