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Bull Exp Biol Med ; 174(2): 221-225, 2022 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-36600040

RESUMO

Cytostatic activity of combretastatin A-4, its 11 analogues, and paclitaxel (Taxacad) was evaluated in vitro on human tumor cells A549 (lung adenocarcinoma) and PC-3 (prostate adenocarcinoma) in order to find the active and stable compound as a promising antitumor agent. 5-(4-Methoxyphenyl)-4-(3,4,5-trimethoxyphenyl)-isoxazole (compound 123124) and 3-(3,4,5-trimethoxyphenyl)-4-(4-methoxyphenyl)-isoxazole (compound 29310186) demonstrated the highest cytostatic activity (IC50≈8×10-9 М). The activity of two other cytotoxic compounds (2E)-1-(7-methoxy-2H-1,3-benzodioxol-5-yl)-3-(4-methoxyphenyl)prop-2-en-1-one (compound 104815) and 4-(3-amino-4-methoxyphenyl)-5-(3,4,5-trimethoxyphenyl)-1H-pyrazole hydrochloride (compound 198732) was close to that of Taxacad: IC50 65×10-9 and 80×10-9 М, respectively, and are also promising active components for the development of antitumor drugs.


Assuntos
Antineoplásicos , Citostáticos , Estilbenos , Masculino , Humanos , Citostáticos/farmacologia , Antineoplásicos/farmacologia , Estilbenos/farmacologia , Isoxazóis , Relação Estrutura-Atividade , Linhagem Celular Tumoral , Ensaios de Seleção de Medicamentos Antitumorais
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