RESUMO
A new class of hybrid chalcones (17a-l &18a-l) was synthesized by Claisen-Schmidt condensation. All compounds were characterized by (1)H NMR, IR and mass spectral analysis and tested for their cytotoxic activity against PC-3 (prostate cancer), HT-29 (colon cancer), B-16 (mouse macrophages) and NCI-H460 (lung cancer) cell lines. Three compounds 18i, 18j and 18l (IC(50)=8.4, 7.9 & 5.9 µM) showed significant activity against PC-3 cell line.
Assuntos
Antineoplásicos/síntese química , Chalcona/análogos & derivados , Animais , Antineoplásicos/uso terapêutico , Antineoplásicos/toxicidade , Apoptose/efeitos dos fármacos , Linhagem Celular Tumoral , Chalcona/uso terapêutico , Chalcona/toxicidade , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Masculino , Camundongos , Neoplasias da Próstata/tratamento farmacológico , Relação Estrutura-AtividadeRESUMO
A series of dihydrofurobenzoxazolin-2(3H)-ones and their derivatives were synthesized. The structures of the compounds have been elucidated by IR, mass, 1H-NMR spectra and elementary analysis. The in vitro activity of these compounds was investigated against Gram-positive and Gram-negative bacteria and also against Candida albicans. 7,7-Dimethyl-7,8-dihydro-furo[2,3-g]benzoxazolin-2(3H)-one (compound 2) proved to be more potent than compound 1. Compound 3 also showed significant activity against all the microbes tested. Compounds 4 and 5 were more effective against Gram-positive bacteria than Gram-negative bacteria but inactive against C. albicans.
