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Synthesis and biological evaluation of fluorinated 3,4-dihydroquinolin-2(1 H )-ones and 2-oxindoles for anti-hepatic fibrosis.

Authors :
Li M
He FS
Ji LS
Gao YT
Zhang X
Yu Z
Fang M
Wu J
Gao YQ
Source :
RSC advances [RSC Adv] 2021 Feb 03; Vol. 11 (11), pp. 5923-5927. Date of Electronic Publication: 2021 Feb 03 (Print Publication: 2021).
Publication Year :
2021

Abstract

( Z )-4-(Iodomethylene)-3-(2,2,2-trifluoroethyl)-3,4-dihydroquinolin-2(1 H )-ones and fluorinated 3,3-disubstituted 2-oxindoles are synthesized and evaluated for anti-hepatic fibrosis. CCK-8 assay indicates that most of the compounds have no obvious cytotoxicity on the human hepatic stellate cells (HSC) cell line. Collagen I and fibrosin expression levels are tested by ELISA, and the results show that several compounds can inhibit the expression of collagen I and fibrosin. Additionally, results from real time-PCR reveal that only one compound can inhibit the expression level of α-SMA, suggesting that this compound can inhibit the activation of the HSC cell line. These studies demonstrate that this compound may be a potential novel drug candidate for anti-hepatic fibrosis (approximately 5-6 lines).<br />Competing Interests: There are no conflicts to declare.<br /> (This journal is © The Royal Society of Chemistry.)

Details

Language :
English
ISSN :
2046-2069
Volume :
11
Issue :
11
Database :
MEDLINE
Journal :
RSC advances
Publication Type :
Academic Journal
Accession number :
35423132
Full Text :
https://doi.org/10.1039/d0ra09430g