Design and synthesis of novel polycycles based on the 3H-pyrrolo/6,7-dihydropyrido[1,2-a]indole scaffold as templates for pharmaceutical development

✍ Scribed by Marco Derudas; Nicolino Pala; Vanna Sanna; Roberto Dallocchio; Alessandro Dessì; Anna Maria Roggio; Mario Sechi

• Publisher: Journal of Heterocyclic Chemistry
• Year: 2011
• Tongue: English
• Weight: 379 KB
• Volume: 48
• Category: Article
• ISSN: 0022-152X
• DOI: 10.1002/jhet.710

✦ Synopsis

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.