| Literature DB >> 26652969 |
Hao Zhang1, Min-Hang Xin1, Xiao-Xiao Xie1, Shuai Mao1, Sai-Jie Zuo1, She-Min Lu2, San-Qi Zhang3.
Abstract
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.Entities:
Keywords: Antitumor activity; PI3K inhibitor; Quinazolin-4(3H)-ones; Synthesis
Mesh：
Substances：
Year: 2015 PMID： 26652969 DOI： 10.1016/j.bmc.2015.11.027
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641