SYNTHESIS OF IMIDAZO[2,1-b][1,3,4]THIADIAZOLE DERIVATIVES AS POSSIBLE BIOLOGICALLY ACTIVE AGENTS.
Acta Pol Pharm
; 73(4): 913-929, 2016 07.
Article
em En
| MEDLINE
| ID: mdl-29648717
ABSTRACT
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).
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Tiadiazóis
/
Anticarcinógenos
/
Imidazóis
/
Antineoplásicos
Limite:
Animals
/
Female
/
Humans
Idioma:
En
Revista:
Acta Pol Pharm
Ano de publicação:
2016
Tipo de documento:
Article