Antiproliferative activity of diarylnaphthylpyrrolidine derivative via dual target inhibition.
Eur J Med Chem
; 188: 111986, 2020 Feb 15.
Article
em En
| MEDLINE
| ID: mdl-31884407
ABSTRACT
Breast cancer is the second leading cause of deaths in women globally. Present communication deals with design and synthesis of a few diarylnaphthyls as possible anti-breast cancer agents. Among the thirty three representatives with significant antiproliferative activity compounds 23 and 50 were quite efficacious against human breast cancer cells. Compound 50 induced apoptosis in both MCF-7 and MDA-MB-231 cells and exerted S phase and G2/M phase arrest respectively via distinct mechanistic pathways. It showed moderate microtubule destabilization. Further, it exhibited DNA topoisomerase-II inhibition effect in MCF-7 cells. It was well tolerable and found safe up to 300 mg/kg dose in Swiss albino mice. The dual action antiproliferative effect of compound 50 is quite interesting and warrants for future development.
Palavras-chave
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Pirrolidinas
/
Moduladores de Tubulina
/
Inibidores da Topoisomerase II
/
Naftalenos
/
Antineoplásicos
Limite:
Animals
/
Female
/
Humans
/
Male
Idioma:
En
Revista:
Eur J Med Chem
Ano de publicação:
2020
Tipo de documento:
Article
País de afiliação:
Índia