Novel cytisine derivatives exert anti-liver fibrosis effect via PI3K/Akt/Smad pathway.

Sheng Tang,Yinghong Li,Yunyang Bao, Zhiting Dai,Tianyu Niu,Kun Wang,Hongwei He,Danqing Song

Bioorganic Chemistry（2019）

引用 15|浏览19

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摘要

•26 new cytisine analogues were gained and evaluated for anti-COL1A1 activity.•5f gave inspiring activity with the inhibitory IC50 value of 12.8 μM.•5f exhibited inhibition effects against a series of fibrogenetic proteins.•5f displayed ideal PK stability and safety profiles.•5f might repress the hepatic fibrogenesis via PI3K/Akt/Smad pathway.

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关键词

Liver fibrosis,Cytisine,Structure-activity relationship,Fibrogenetic protein,COL1A1

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