Discovery of Fluoroquinolone derivatives as potent,selective inhibitors of PI3Kγ

摘要：

　　Phosphoinositide 3-kinase(PI3K)is an attractive target to potentially treat a range of disease stales as illustrated by more than 15 inhibitors now in clinical trials.We disclose herein the discovery of a new class of fluoroquinolone derivatives having improved potency toward PI3K.The activity of the compound A3 as an inhibitor of PI3K was further investigated in human lumors cells Notably,the compound A3 with potent inhibitory activity was low toxic.By compoutational docking studies,it was predicted that like CAL-101,a known small-inhibitor of PI3K.compound A3 was tightly embedded into the ATP binding pocket with H bonds and π-cation interactions.

关键词： Fluoroquinolone derivatives Computational docking PI3K inhibitor Antitumor activity

作者: Shao Sha Hong-Wei Han Fei Gao Tian-Bao Liu Zhen Li Chi Xu Wei-Qing Zhong Hai-Liang Zhu

作者单位: State Key Laboratory of Pharmaceutical Biotechnology,Nanjing University,Nanjing 210093,P.R China School of Pharmacy,Second Military Medical University,Shanghai 200433,P.R.China State Key Laboratory of Pharmaceutical Biotechnology,Nanjing University,Nanjing 210093,P.R China;Sch

会议类型: 国内会议

会议名称: 第八届国际分子模拟与信息技术应用学术会议

会议地点: 大连

会议语种:英文

页码: 310-330

在线出版日期: 2016-09-24（万方平台首次上网日期，不代表论文的发表时间）