Design, synthesis and biological evaluation of 2-(phenoxymethyl)-5-phenyl-1,3,4-oxadiazole derivatives as anti-breast cancer agents.
1,3,4-Oxadiazoles
Breast cancer
Estrogen receptor
Molecular docking
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 Apr 2019
15 Apr 2019
Historique:
received:
01
12
2018
revised:
09
02
2019
accepted:
10
02
2019
pubmed:
25
2
2019
medline:
23
4
2019
entrez:
25
2
2019
Statut:
ppublish
Résumé
Structural based molecular docking approach revealed the findings of 2-(phenoxymethyl) -5-phenyl-1,3,4-oxadiazole derivatives. The compounds (7a-o) were synthesized and characterized well by using conventional methods. The compounds, 7b and 7m were reconfirmed through single crystal XRD analysis. The synthesized compounds (7a-o) were evaluated their antiproliferative activities against MCF-7 and MDA-MB-453. Furthermore, Lipinski's rule of five and pharmacokinetic properties were predicted for the test compounds. These results demonstrate that the compounds 7b and 7d exhibit more potent cytotoxicity and 7d exhibits dose-dependent activity and reduced cell viability. Further, the mechanism of action for the induced apoptosis was observed through morphological changes and western blotting analysis. These findings may furnish the lead for further development.
Identifiants
pubmed: 30798049
pii: S0223-5234(19)30147-3
doi: 10.1016/j.ejmech.2019.02.033
pii:
doi:
Substances chimiques
Antineoplastic Agents
0
Oxadiazoles
0
1,3,4-oxadiazole
20O2F20OUR
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
1-10Informations de copyright
Copyright © 2019 Elsevier Masson SAS. All rights reserved.