RESUMO
A series of 2-oxindole derivatives were synthesized and evaluated for cytotoxic activity against different human and murine cancer cell lines and cancer chemopreventive activity. Among the tested compounds VS-06, 08, 12 and 17 displayed cytotoxic activity in the range of 5.0 to 8.5 pM against human T-lymphocyte cells (CEM). Results showed that molecules with electron withdrawing substituent at 4 position of N-phenylacetamide group exhibited an increase in activity against the human tumor cell line CEM. The cancer chemo- preventive effect of VS-01 (IC50 = 451 nM) displayed equipotent activity in comparison to standard oleanolic acid (IC50 = 449 nM).
Assuntos
Anticarcinógenos/síntese química , Antineoplásicos/síntese química , Animais , Anticarcinógenos/farmacologia , Antineoplásicos/farmacologia , Linhagem Celular Tumoral , Humanos , Relação Estrutura-AtividadeRESUMO
A series of 2-(4-methylbenzyl)-5,6-substituted-imidazo[2,1-b][1,3,4]thiadiazole derivatives were synthesized, characterized and evaluated for antiproliferative activity and cancer chemopreventive activity. Results showed that molecules with formyl and thiocyanate substiments at the 5 position exhibited an increase in activity against the full panel of 60 human tumor cell lines at a minimum of five concentrations at 10-fold dilutions. Derivative 22 displayed significant in vino anticancer activity against colon cancer (MID GI50 = 0.75 µM). The cancer chemopreventive effect of 19 (IC50 = 489 nM) was almost equipotent to standard oleanolic acid (IC50 = 449 nM).