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

Publication date: Available online 22 November 2015
Source:Bioorganic & Medicinal Chemistry
Author(s): Hao Zhang, Min-Hang Xin, Xiao-Xiao Xie, Shuai Mao, Sai-Jie Zuo, She-Min Lu, San-Qi Zhang
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.

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