Discovery of a series of N-(5-(quinolin-6-yl)pyridin-3-yl)benzenesulfonamides as PI3K/mTOR dual inhibitors

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• 作者：Jiankang Zhang^b ; Xiaoqing Lv^a ; ^{lxqd1@126.com} ; Xiaodong Ma^c ; Yongzhou Hu^d
• 关键词：PI3K ; mTOR ; Cancer ; Inhibitor
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：15 February 2017
• 年：2017
• 卷：127
• 期：Complete
• 页码：509-520
• 全文大小：1786 K
• 卷排序：127

文摘

Most of the substituted quinolines displayed potent activities against PI3Kα. 3-(2-Morpholinoacetamido)quinoline (17e) showed the most potency against PC3 cells. 17e exhibited strong inhibitory effect on class I PI3Ks, mTOR and pAkt(Ser473). 17e showed acceptable pharmacokinetic properties in vivo.