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Synthesis and evaluation of antiproliferative effect of amidino substituted heterocyclic compounds "in vitro"

Amidino substituted heterocyclic compounds are widely investigated on their biological activity1. Organic dications and monocations that bind to the DNA as intercalators or "groove binders" exibit biological activities that range from effectiveness against opportunistic infections to anticaner properties.2 The purpose of this study was to synthesized three cyclic heterocyclic compound and investigate the effects on proliferation of different human tumor cell lines, as well as on normal (diploid) human fibroblasts (control cell line). The experiments were carried out on 6 human cell lines, 5 of which are derived from 5 cancer types and one normal, fibroblast cell line. The following cell lines were used: HeLa (cervical carcinoma), MCF-7 (breast carcinoma), SW 620 (colon carcinoma), MiaPaCa-2 (pancreatic carcinoma), Hep-2 (laryngeal carcinoma) and WI 38 (diploid fibroblasts). All compounds produced markedly strong antiproliferative effect and were cytotoxic to all cell lines.3, 4 LITERATURE: 1. J.E. Hall, J.E. Kerrigan, K. Ramachandran, B.C. Bender, J.P. Stanko, S.K. Jones, D.A. Patrick, R.R. Tidwell, Antimicrob Agents Chemother, 1998, 42, 666-674 2. R.R. Tidwell and D.W. Boykin, Dicationic DNA Minor Groove Binders as Antimicrobial Agents, in Small Molecule DNA and RNA Binders ; From Synthesis to Nucleic Acid Complexes, Ed. By M. Demeunynck, C. Bailly, and W.D. Wilson, Wiley-VCH, New York, 2003, vol. 2, 416-460 3. T. Mossman, Immunol 1983, 65, 55­63. 4. M.R.Boyd, D.P. Kenneth, Drug Dev Res 1995, 34, 91-109.

amidines; heterocyclic compounds; biological activity

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