Artículos de revistas
Effect of 3,4-ethylenedioxy-extension of thiophene core on the DNA/RNA binding properties and biological activity of bisbenzimidazole amidines
Fecha
2009Registro en:
BIOORGANIC & MEDICINAL CHEMISTRY, v.17, n.6, p.2544-2554, 2009
0968-0896
10.1016/j.bmc.2009.01.071
Autor
STOLIC, Ivana
MISKOVIC, Katarina
MAGDALENO, Anahi
SILBER, Ariel Mariano
PIANTANIDA, Ivo
BAJIC, Miroslav
GLAVAS-OBROVAC, Ljubica
Institución
Resumen
Novel bisbenzimidazoles (4-6), characterized by 3,4-ethylenedioxy-extension of thiophene core, revealed pronounced affinity and strong thermal stabilization effect toward ds-DNA. They interact within ds-DNA grooves as dimmers or even oligomers and agglomerate along ds-RNA. Compounds 4-6 have shown moderate to strong antiproliferative effect toward panel of eight carcinoma cell lines. Compound 5 displayed the best inhibitory potential and in equitoxic concentration (IC(50) = 1 x 10 (6) M) induced accumulation of cells in G2/M phase after 48 h of incubation. Fluorescence microscopy showed that 5 entered into live HeLa cells within 30 min, but did not accumulate in nuclei even after 2.5 h. Compound 5 inhibited the growth of Trypanosome cruzi epimastigotes (IC(50) = 4.3 x 10 (6) M). (C) 2009 Elsevier Ltd. All rights reserved.