Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1369411 | Bioorganic & Medicinal Chemistry Letters | 2016 | 6 Pages |
Abstract
A series of 4,6-disubstituted quinazoline derivatives as potential PI3K inhibitors were designed and synthesized. All compounds exhibited significant anti-proliferative activities against HCT-116 and MCF-7 cell lines, and compounds A7, A9, and A11 displayed the most potent anti-proliferative activity against the HCT-116. Further PI3K inhibitory activity evaluation showed that compound A7 displayed high potency against PI3K enzymes. The in vivo anti-tumor study showed compound A7 can efficaciously inhibit tumor growth in a mice S-180 model. These results suggest that our designed compounds can serve as potent PI3K inhibitors and effective antitumor agents.
Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Yuan-Yuan Hei, Minhang Xin, Hao Zhang, Xiao-Xiao Xie, Shuai Mao, San-Qi Zhang,