engleski

Effect of 3, 4-Ethylenedioxy- Extension of Thiophene Core on the DNA/RNA Binding Properties and Biological Activity of Bis-Benzimidazole Amidines

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 (IC50 = 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 T. cruzi epimastigotes (IC50 = 4.3 x 10– 6 M).

benzimidazole amidine ; DNA/RNA binding ; antiproliferative activity ; antiparasitic activity

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