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