Identification of 3-amidoquinoline derivatives as PI3K/mTOR dual inhibitors with potential for cancer therapy
作者： Jiankang Zhang , Xiaodong Ma , Xiaoqing Lv , Ming Li , Yanmei Zhao
DOI: 10.1039/C6RA26971K
关键词:
摘要: 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) anti-proliferative 1 μM). The representative compound 15a can significantly inhibit other class I PI3Ks, mTOR phosphorylation pAkt(Ser473) at low nanomolar level, suggesting that was a inhibitor. Moreover, displayed favorable pharmacokinetic properties in vivo.
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