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Published: Kem. Ind. 60 (5) (2011) 277–288
Paper reference number: KUI-22/2010
Paper type: Review
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Diarylamidines: Design, Interaction with DNA and Biological Activity

I. Stolić and M. Bajić


Diarylamidines are a group of biologically active compounds that are more than half a century used for treatment of parasitic diseases. Although the biological mechanism of action has not yet been fully explained it was found that the biological activity of compounds of this class is based on their binding in a small groove of DNA. Therefore, the compounds of this class, originally developed for the purpose of finding parasitic drugs, over time are recognized as potential drugs with broad application (e. g. anti-HIV opportunistic infections or tumours) based on their interaction with DNA – the primary genetic material. The occurrence of resistance and some associated adverse consequences prompted the research and development of new effective drugs and finding their mechanism of action at the molecular level. In the first part of this work, basic concepts are given accompanied by selected examples of this class of compounds.

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diarylamidines, B-DNA minor groove, biological activity