Discovery of Matrinic Thiadiazole Derivatives as a Novel Family of Anti-Liver Fibrosis Agents via Repression of the TGFβ/Smad Pathway

Discovery of Matrinic Thiadiazole Derivatives as a Novel Family of Anti-Liver Fibrosis Agents via Repression of the TGFβ/Smad Pathway

A series of novel matrinic thiadiazole derivatives were designed, synthesized and evaluated for their inhibitory effect on COL1A1 promotor. The SAR indicated that: (i) the introduction of a thiadiazole on the 11-side chain was beneficial for activity; (ii) a 12-N-benzyl moiety was favorable for acti...

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Bibliographic Details
Main Authors: Tianyu Niu, Weixiao Niu, Yunyang Bao, Ting Liu, Danqing Song, Yinghong Li, Hongwei He
Format: Article
Language:English
Published: MDPI AG 2018-07-01
Series:Molecules
Subjects:
liver fibrosis
matrinic
thiadiazole
structure-activity relationship
COL1A1
TGFβ/Smad pathway
Online Access:http://www.mdpi.com/1420-3049/23/7/1644

Internet

http://www.mdpi.com/1420-3049/23/7/1644

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