Novel 4-Acrylamido-Quinoline Derivatives as Potent PI3K/mTOR Dual Inhibitors: The Design, Synthesis, and in vitro and in vivo Biological Evaluation

A novel structural series of quinoline derivatives were designed, synthesized and biologically evaluated as PI3K/mTOR dual inhibitors upon incorporation of C-4 acrylamide fragment. Consequently, all of them exerted remarkable inhibition against PI3Kα with IC50 values ranging from 0.50 to 2.03 nM. Be...

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Bibliographic Details
Main Authors: Xiaodong Ma, Li Shen, Jiankang Zhang, Guoqiang Liu, Shuyu Zhan, Baoyue Ding, Xiaoqing Lv
Format: Artigo
Language:Inglês
Published: Frontiers Media S.A. 2019-04-01
Series:Frontiers in Chemistry
Subjects:
4-acrylamido-quinolines
PI3K/mTOR dual inhibitors
anti-proliferative activity
PI3K/Akt/mTOR signaling
metabolic stability
PK study
Online Access:https://www.frontiersin.org/article/10.3389/fchem.2019.00236/full
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