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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

DNA Binders: 1. Evaluation of DNA-Interactive Ability, Design, and Synthesis of Novel Intercalating Agents

Author(s): Mario Sechi, Marco Derudas, Roberto Dallocchio, Alessandro Dessì, Alessia Cosseddu and Giuseppe Paglietti

Volume 6, Issue 1, 2009

Page: [56 - 62] Pages: 7

DOI: 10.2174/157018009787158472

Price: $65

Abstract

Previously, we designed and synthesized the 2,3,6,7-tetrahydro-1H-pyrrolo[1,2-a]indole-1,8(5H)-dione as a versatile structural platform to be functionalized to obtain potential DNA-interactive agents by intercalation and/or reversible enzyme inhibition. Herein, we report an alternative synthetic route for the preparation of this heterocyclic template as well as the synthesis of an its “two-armed” derivative. Also, a computational docking study to investigate the possible DNA-binding mode of well-known binders and title compound was performed.

Keywords: DNA binders, Docking, Intercalation, Two-armed derivatives, 2,3,6,7-Tetrahydro-1H-pyrrolo[1,2-a]indole- 1, 8(5H)-dione


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