Design, synthesis, and anti-proliferative evaluation of new quinazolin-4(3H)-ones as potential VEGFR-2 inhibitors.
Antineoplastic Agents
/ chemical synthesis
Cell Proliferation
/ drug effects
Dose-Response Relationship, Drug
Drug Design
Drug Screening Assays, Antitumor
Humans
Molecular Docking Simulation
Molecular Structure
Protein Kinase Inhibitors
/ chemical synthesis
Quinazolinones
/ chemical synthesis
Structure-Activity Relationship
Tumor Cells, Cultured
Vascular Endothelial Growth Factor Receptor-2
/ antagonists & inhibitors
Anticancer
Molecular docking
Quinazolin-4(3H)-one
VEGFR-2
Journal
Bioorganic & medicinal chemistry
ISSN: 1464-3391
Titre abrégé: Bioorg Med Chem
Pays: England
ID NLM: 9413298
Informations de publication
Date de publication:
01 01 2021
01 01 2021
Historique:
received:
17
07
2020
revised:
03
11
2020
accepted:
06
11
2020
pubmed:
21
11
2020
medline:
31
7
2021
entrez:
20
11
2020
Statut:
ppublish
Résumé
Inhibiting VEGFR-2 has been set up as a therapeutic strategy for treatment of cancer. Thus, nineteen new quinazoline-4(3H)-one derivatives were designed and synthesized. Preliminary cytotoxicity studies of the synthesized compounds were evaluated against three human cancer cell lines (HepG-2, MCF-7 and HCT-116) using MTT assay method. Doxorubicin and sorafenib were used as positive controls. Five compounds were found to have promising cytotoxic activities against all cell lines. Compound 16
Identifiants
pubmed: 33214036
pii: S0968-0896(20)30702-1
doi: 10.1016/j.bmc.2020.115872
pii:
doi:
Substances chimiques
Antineoplastic Agents
0
Protein Kinase Inhibitors
0
Quinazolinones
0
KDR protein, human
EC 2.7.10.1
Vascular Endothelial Growth Factor Receptor-2
EC 2.7.10.1
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
115872Informations de copyright
Copyright © 2020 Elsevier Ltd. All rights reserved.