Discovery of a 2,4-diphenyl-5,6-dihydrobenzo(h)quinolin-8-amine derivative as a novel DNA intercalating topoisomerase IIα poison.
Amines
/ chemical synthesis
Antineoplastic Agents
/ chemical synthesis
Cell Proliferation
/ drug effects
DNA Topoisomerases, Type II
/ metabolism
Dose-Response Relationship, Drug
Drug Discovery
Drug Screening Assays, Antitumor
Humans
Molecular Structure
Structure-Activity Relationship
Topoisomerase II Inhibitors
/ chemical synthesis
Tumor Cells, Cultured
2,4,6-Triarylyridines
5,6-Dihydrobenzo(h)Quinolin-8-amine
Antiproliferative activity
Structure-activity relationship
Topo IIα poison inhibitor
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:
15 Dec 2021
15 Dec 2021
Historique:
received:
13
07
2021
revised:
04
09
2021
accepted:
17
09
2021
pubmed:
2
10
2021
medline:
27
1
2022
entrez:
1
10
2021
Statut:
ppublish
Résumé
Several anticancer agents have been developed and innovative approaches have been made toward cancer type-specific medicines for cancer treatment. As a continuous effort to develop potential chemotherapeutic agents, a novel series of 2,4-diphenyl-5,6-dihydrobenzo(h)quinolin-8-amines containing amino groups, hydroxyphenyl and fluorine functionalities were designed and synthesized. The compounds were evaluated for topo IIα inhibitory and cytotoxicity against HCT15, and HeLa human cancer cell lines. Among synthesized thirty compounds, the majority exhibited strong topo IIα inhibition and anti-proliferation against HCT15 colorectal adenocarcinoma cell line. The structure-activity relationship study revealed that compounds with -CF
Identifiants
pubmed: 34597897
pii: S0223-5234(21)00709-1
doi: 10.1016/j.ejmech.2021.113860
pii:
doi:
Substances chimiques
Amines
0
Antineoplastic Agents
0
Topoisomerase II Inhibitors
0
DNA Topoisomerases, Type II
EC 5.99.1.3
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
113860Informations de copyright
Copyright © 2021 Elsevier Masson SAS. All rights reserved.
Déclaration de conflit d'intérêts
Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.