Synthesis, biological evaluation and anti-proliferative mechanism of fluorine-containing proguanil derivatives.

Di Xiao, Zhicheng Lu,Zhiren Wang,Sichun Zhou,Mengru Cao,Jun Deng,Xin Hu,Mei Peng,Caimei He,Jingtao Wu,Simeng Xu,Huihui Zhang,Cangcang Xu,Wei Wang,Aiying Guan,Xiaoping Yang

Bioorganic & Medicinal Chemistry（2020）

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摘要

•13 new fluorine-containing proguanil derivatives were designed and synthesized.•Derivatives with trifluoromethyl phenyl or n-heptane substitutions exert a strongest antiproliferative activities.•Derivative 7a blocks the tumor cell growth by influencing AMPK-mTOR signal pathway.

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关键词

Biguanides,Fluorine-containing compounds,Anti-proliferative,AMPK

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