Identification of 3-amidoquinoline derivatives as PI3K/mTOR dual inhibitors with potential for cancer therapy. Issue 4 (12th January 2017)

• Record Type: Journal Article
• Authors: Zhang, Jiankang; Ma, Xiaodong; Lv, Xiaoqing; Li, Ming; Zhao, Yanmei; Liu, Guoqiang; Zhan, Shuyu
• Is Part Of: RSC advances. Volume 7:Issue 4(2017)
• Page Start: 2342
• Page End: 2350
• Publication Date: 2017-01-12
• Subjects: Chemistry -- Periodicals; 540.5
• DOI: 10.1039/c6ra26971k
• Languages: English
• ISSNs: 2046-2069

Abstract

Abstract : A new series of 3-amidoquinoline derivatives were designed, synthesized and evaluated as PI3K/mTOR dual inhibitors. Abstract : A new series of 3-amidoquinoline derivatives were designed, synthesized and evaluated as PI3K/mTOR dual inhibitors. Among them, five compounds showed potent PI3Kα inhibitory activities (IC50 < 10 nM) and anti-proliferative activities (IC50 < 1 μM). The representative compound15a can significantly inhibit other class I PI3Ks, mTOR and phosphorylation of pAkt(Ser473) at low nanomolar level, suggesting that15a was a potent PI3K/mTOR dual inhibitor. Moreover, 15a displayed favorable pharmacokinetic properties in vivo .