Discovery of new quinazolin-4(3H)-ones as VEGFR-2 inhibitors: Design, synthesis, and anti-proliferative evaluation.
Antineoplastic Agents
/ chemical synthesis
Cell Proliferation
/ drug effects
Dose-Response Relationship, Drug
Drug Discovery
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
Antiangiogenesis
Antiproliferative
Docking studies
Quinazolin-4(3H)-one
VEGFR-2
Journal
Bioorganic chemistry
ISSN: 1090-2120
Titre abrégé: Bioorg Chem
Pays: United States
ID NLM: 1303703
Informations de publication
Date de publication:
12 2020
12 2020
Historique:
received:
16
07
2020
revised:
14
09
2020
accepted:
12
10
2020
pubmed:
1
11
2020
medline:
17
6
2021
entrez:
31
10
2020
Statut:
ppublish
Résumé
Sixteen novel quinazoline-based derivatives were designed and synthesized via modification of the VEGFR-2 reported inhibitor 7 in order to increase the binding affinity of the designed compounds to the receptor active site. The designed compounds were evaluated for their VEGFR-2 inhibitory effects. Inhibiting VEGFR-2 has been set up as a therapeutic strategy for treatment of cancer. The bioactivity of the new compounds was performed against HepG-2, MCF-7 and HCT-116 cell lines. Doxorubicin and sorafenib were used as positive controls. Compound 18
Identifiants
pubmed: 33128967
pii: S0045-2068(20)31678-3
doi: 10.1016/j.bioorg.2020.104380
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
104380Informations de copyright
Copyright © 2020 Elsevier Inc. All rights reserved.