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New Naphthofurans Derivatives : Biological Evaluations and Interactions with ct-DNA

Intercalation of aromatic compounds in double stranded (ds) nucleic acids is of paramount significance for many biologically and medicinally important interactions [1]. On the other hand, amidine derivatives are among the very few small molecules that efficiently inhibit of Rev-RRE binding [2] In the reaction of condensation of methyl E-3-(5-formyl-2-furyl)-2-phenylacrylate with corresponding 4-amidino substituted o-phenylenediamines [3], were prepared new subsituted benzimidazoles which gave in the reaction of photodehydrocyclization [4] desired compound 1. Therefore, the new amidino substituted compound 2 was prepared by Pinner reaction [3] converted into naphtho[2, 1-b]furan derivative by photodehydrocyclization.[4] The purpose of this study was to synthesized novel heterocyclic compounds and investigate the effects on proliferation of different human tumor cell lines, as well as on normal (diploid) human fibroblasts (control cell line) and to study their interactions with ct-DNA and RNA.[5] Novel compounds 1 and 2 were fully spectroscopicaly characterized. Interactions of compounds 1 and 2 with ct-DNA and RNA were studied by spectroscopic titrations (UV/Vis and f1uorimetric) and thermal denaturation experiments. 1. M. Demeunyvnk, C. Baily, W. D. Wilson ; DNA and RNA binders, Wiley-VCH, Weinheim, 2002 2. K. Li, G. Xiao, T. Rigl, A. Kumar, D. W. Boykin, W. D. Wilson, In Structure, Motion, Interaction and Expression of Biological Macromolecules, (Eds. ; R.H. Sarma, M.H. Sarma), Adenine Press, 1998, 137 3. Patrick, D. A., Boykin, D. W., Wilson, W. D., Tanious, F. A., Spychala, J., Bender, B. C., Hall, J. E., Dykstra, C. C., Ohemeng, K. A., Tidwell, R.R., Eur. J. Med. Chem., 32 (1997) 781-793 4. Starčević, K., Boykin, D. W., Karminski-Zamola, G., Heterocyclic Comm., 8 (2002) 221-226 5. K. Starčević, G. Karminski-Zamola, I. Piantanida, M. Žinić, L. Šuman, M. Kralj, J. Am. Chem. Soc., 127 (2005) 1074-1075

naphthofurans; amidines; benzimidazoles; interactions with DNA

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