N-Substituted-4-phenylphthalazin-1-amine-derived VEGFR-2 inhibitors: Design, synthesis, molecular docking, and anticancer evaluation studies.
Amines
/ chemical synthesis
Antineoplastic Agents
/ chemical synthesis
Cell Line, Tumor
Cell Proliferation
/ drug effects
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
Humans
Molecular Structure
Phthalazines
/ chemical synthesis
Protein Kinase Inhibitors
/ chemical synthesis
Structure-Activity Relationship
Vascular Endothelial Growth Factor Receptor-2
/ antagonists & inhibitors
4-phenylphthalazin-1-amine
VEGFR-2 inhibitors
anticancer agents
molecular docking
Journal
Archiv der Pharmazie
ISSN: 1521-4184
Titre abrégé: Arch Pharm (Weinheim)
Pays: Germany
ID NLM: 0330167
Informations de publication
Date de publication:
Mar 2021
Mar 2021
Historique:
received:
26
06
2020
revised:
04
09
2020
accepted:
24
10
2020
pubmed:
17
11
2020
medline:
7
10
2021
entrez:
16
11
2020
Statut:
ppublish
Résumé
In accordance with the significant impetus of the discovery of potent vascular endothelial growth factor receptor 2 (VEGFR-2) inhibitors, herein, we report the design, synthesis, and anticancer evaluation of 12 new N-substituted-4-phenylphthalazin-1-amine derivatives against HepG2, HCT-116, and MCF-7 cells as VEGFR-2 inhibitors. The results of the cytotoxicity investigation indicated that HCT-116 and MCF-7 were the most sensitive cell lines to the influence of the newly synthesized derivatives. In particular, compound 7a was found to be the most potent derivative among all the tested compounds against the three cancer cell lines, HepG2, HCT116, and MCF-7, with IC
Identifiants
pubmed: 33197080
doi: 10.1002/ardp.202000219
doi:
Substances chimiques
Amines
0
Antineoplastic Agents
0
Phthalazines
0
Protein Kinase Inhibitors
0
phthalazine
91Y28DM24N
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
e2000219Informations de copyright
© 2020 Deutsche Pharmazeutische Gesellschaft.
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