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Bioorg Med Chem Lett ; 30(23): 127554, 2020 12 01.
Artigo em Inglês | MEDLINE | ID: mdl-32950616

RESUMO

The occurrence and development of cervical cancer threaten women's life and health, HPV-induced cervical cancer is a major health issue among women. We synthesized three Rhopaladins' analogue (E)-2-aroyl-4-(4-fluorobenzylidene)-5-oxopyrrolidines via a tandem Ugi 4CC/SN cyclization with pyrrolidone as a core structure. In addition, the cytotoxicity of these new compounds in the cervical cancer cell line CaSki was studied by MTT assay. And then we chose one to research the apoptosis and the expression of E6/E7 mRNA in CaSki cells. The results indicated that the new compound can not only inhibited the proliferation of CaSki in dose-dependent and time-dependent manners but also induced the apoptosis, which may be related to the down-regulation of E6/E7 mRNA expression.


Assuntos
Antineoplásicos/farmacologia , Apoptose/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Pirrolidinonas/farmacologia , RNA Mensageiro/metabolismo , Neoplasias do Colo do Útero/tratamento farmacológico , Antineoplásicos/síntese química , Linhagem Celular Tumoral , Ciclização , Regulação para Baixo/efeitos dos fármacos , Ensaios de Seleção de Medicamentos Antitumorais , Feminino , Humanos , Proteínas E7 de Papillomavirus/genética , Pirrolidinonas/síntese química
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