Discovery and evaluation of phenacrylanilide derivatives as novel potential anti-liver fibrosis agents

Autor:	Lin, Yue, Taixiong, Xue, Xingping, Su, Zhihao, Liu, Hongyao, Liu, Zui, Tan, Cailing, Gan, Yuting, Xie, Tinghong, Ye
Rok vydání:	2022
Předmět:	Liver Cirrhosis Transforming Growth Factor beta1 Pharmacology Mice Organic Chemistry Drug Discovery Hepatic Stellate Cells Animals General Medicine Carbon Tetrachloride Fibrosis Fibronectins
Zdroj:	European Journal of Medicinal Chemistry. 242:114685
ISSN:	0223-5234
Popis:	Liver fibrosis is characterized by the excessive deposition of extracellular matrix components and results from chronic liver injury. At present, there is no approved drug for the treatment of liver fibrosis by the Food and Drug Administration. Here, we have reported a series of novel compounds with phenacrylanilide scaffolds that potently inhibit the transfer growth factor β1 (TGF-β1)-induced activation of LX-2, a hepatic stellate cell (HSC) line. Among them, compound 42 suppressed TGF-β1-induced upregulation of fibrotic markers (α-SMA and fibronectin) and showed excellent safety in vitro. Furthermore, in a carbon tetrachloride (CCl
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fb2698239f154d8d0eef67b708d33d9a https://doi.org/10.1016/j.ejmech.2022.114685 Zobrazit plný text záznamu Full Text from ScienceDirect