Derudas, Marco and Pala, Nicolino and Sanna, Vanna and Dallocchio, Roberto and Dessì, Alessandro and Roggio, Anna Maria and Sechi, Mario (2011) Design and synthesis of novel polycycles based on the 3H-Pyrrolo/6,7-Dihydropyrido[1,2-a]indole scaffold as templates for pharmaceutical development. Journal of Heterocyclic Chemistry, Vol. 48 (5), p. 1161-1168. ISSN 0022-152X. eISSN 1943-5193. Article.
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In the course of our work aimed at developing novel heterocycles of pharmaceutical interest, we designed and synthesized several polycyclic templates as potential substrates to be used in drug design. We obtained a set of condensed ring systems as versatile structural platforms to generate potential DNA-interactive agents and/or reversible inhibitors of enzymes such as topoisomerases, poly(ADPribose) polymerase-1 (PARP-1), telomerase, and, in particular, cyclin dependent kinases. Herein, we report the design, synthesis, structural investigation, and preliminary DNA-binding affinity of these heteroaromatic systems.
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