Discovery of novel quinazolinone derivatives as potential anti-HBV and anti-HCC agents.
Antineoplastic Agents
/ chemical synthesis
Antiviral Agents
/ chemical synthesis
Apoptosis
/ drug effects
Carcinoma, Hepatocellular
/ pathology
Cell Line, Tumor
Dose-Response Relationship, Drug
Drug Design
Drug Resistance, Viral
/ drug effects
Hepatitis B virus
/ drug effects
Humans
Liver Neoplasms
/ pathology
Quinazolinones
/ chemical synthesis
Virus Replication
/ drug effects
Anti-HBV agents
Anti-HCC activity
Non-nucleoside
Quinazolinone derivatives
Journal
European journal of medicinal chemistry
ISSN: 1768-3254
Titre abrégé: Eur J Med Chem
Pays: France
ID NLM: 0420510
Informations de publication
Date de publication:
01 Nov 2020
01 Nov 2020
Historique:
received:
14
09
2019
revised:
10
06
2020
accepted:
11
06
2020
pubmed:
14
8
2020
medline:
20
4
2021
entrez:
14
8
2020
Statut:
ppublish
Résumé
As a continuation of earlier works, a series of novel quinazolinone derivatives (5a-s) were synthesized and evaluated for their in vitro anti-HBV and anti-hepatocellular carcinoma cell (HCC) activities. Among them, compounds 5j and 5k exhibited most potent inhibitory effect on HBV DNA replication in both drug sensitive and resistant (lamivudine and entecavir) HBV strains. Interestingly, besides the anti-HBV effect, compound 5k could significantly inhibit the proliferation of HepG2, HUH7 and SK- cells, with IC
Identifiants
pubmed: 32791397
pii: S0223-5234(20)30553-5
doi: 10.1016/j.ejmech.2020.112581
pii:
doi:
Substances chimiques
Antineoplastic Agents
0
Antiviral Agents
0
Quinazolinones
0
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
112581Informations de copyright
Copyright © 2020 Elsevier Masson SAS. All rights reserved.
Déclaration de conflit d'intérêts
Declaration of competing interest The authors declared that there was no conflicts of interest to this work. We declare that we do not have any commercial or associative interest that represents a conflict of interest in connection with the work submitted.