engleski

SYNTHESIS AND BIOLOGICAL ACTIVITY OF NEW AMIDINO-SUBSTITUTED-BENZIMIDAZOLES AND AMIDINO-SUBSTITUTED-BENZIMIDAZO [1, 2-a]QUINOLINES AS HYDROCHLORIDE SALTS

Amidino substituted heterocyclic compounds exhibit antitumor activity, and serve as intercalators on DNA and inhibitors of topoisomerase II1, or as "groove binders" 2. The effects of several compounds on proliferation of different human tumor cell lines, as well as on normal (diploid) human fibroblasts (control cell line) were investigated. The experiments were carried out on the following cell lines: HeLa (cervical carcinoma), MCF-7 (breast carcinoma), SW 620 (colon carcinoma), MiaPaCa-2 (pancreatic carcinoma), Hep-2 (laryngeal carcinoma) and WI 38 (diploid fibroblasts).3, 4 All new prepared compounds had markedly differential antiproliferative activity among the panel cell lines, but interestingly, all compounds showed potent inhibitory effect on HeLa cell line. LITERATURE: 1. E. P. Vivas-Mejía et all ; Molecular and Cellular Biochemistry 1997, 177, 69. 2. C. Kus, D. W. Boykin, H. Göker ; Heterocyclic Comm. 2002, 8, 3, 215. 3. M. R. Boyd, D. P. Kenneth ; Drug Dev Res. 1995, 34, 91-109. 4. Mossman, T ; Immunol. 1983, 65, 55­63.

benzimidazoles; amidines; quinolines

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