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

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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DOI: 10.1002/jhet.710

Abstract

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.

Item Type:	Article
ID Code:	6176
Status:	Published
Refereed:	Yes
Uncontrolled Keywords:	CDKs inhibitors, novel heterocycles, HOMO and LUMO coefficients, DNA-interactive agents
Subjects:	Area 03 - Scienze chimiche > CHIM/08 Chimica farmaceutica
Divisions:	002 Altri enti e centri di ricerca del Nord Sardegna > Porto Conte Ricerche, Alghero 002 Altri enti e centri di ricerca del Nord Sardegna > CNR-Consiglio Nazionale delle Ricerche > Istituto di chimica biomolecolare, Sassari 001 Università di Sassari > 01 Dipartimenti > Scienze del farmaco
Publisher:	Wiley / Blackwell
ISSN:	0022-152X
eISSN:	1943-5193
Copyright Holders:	© 2011 HeteroCorporation
Deposited On:	23 Jun 2011 16:29

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