Effect of 3,4-ethylenedioxy-extension of thiophene core on the DNA/RNA binding properties and biological activity of bisbenzimidazole amidines |
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| Authors: | Ivana Stoli? Katarina Mi?kovi? Anahi Magdaleno Ariel Mariano Silber Ivo Piantanida Miroslav Baji? Ljubica Glava?-Obrovac |
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| Institution: | 1. Department of Chemistry and Biochemistry, Faculty of Veterinary Medicine, University of Zagreb, Heinzelova 55, 10000 Zagreb, Croatia;2. Department of Medical Chemistry and Biochemistry, School of Medicine, J.J. Strossmayer University of Osijek, 31000 Osijek, Croatia;3. Department of Parasitology, Institute of Biomedical Sciences, University of São Paulo, São Paulo, Brazil;4. Division of Organic Chemistry and Biochemistry, Ru?er Bo?kovi? Institute, Zagreb, Croatia |
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| Abstract: | 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 × 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 (IC50 = 4.3 × 10?6 M). |
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