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Bioorg Med Chem ; 14(21): 7282-92, 2006 Nov 01.
Artigo em Inglês | MEDLINE | ID: mdl-16843672

RESUMO

A series of novel 2,4-diaminopyrimido[4,5-b]indol-6-ols has been synthesized and the in vitro cytotoxic activities were evaluated against four human cancer cell lines originating from solid tumors. An increase in activity was observed when a heteroaromatic ring was annulated on side g of the pyrimido[4,5-b]indole system to give compounds with activities comparable to ellipticine and cisplatin. To understand the experimental cytotoxic activities, QSAR investigations were performed, which showed a very good linearity between the experimental and predicted IC(50).


Assuntos
Antineoplásicos/síntese química , Antineoplásicos/farmacologia , Pirimidinas/síntese química , Pirimidinas/farmacologia , Antineoplásicos/química , Espectroscopia de Ressonância Magnética , Espectrometria de Massas , Pirimidinas/química , Relação Quantitativa Estrutura-Atividade , Espectrofotometria Infravermelho
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