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, Giuseppe Paglietti

Journal Name: Letters in Drug Design & Discovery

Volume 6 , Issue 1 , 2009

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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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Article Details

Year: 2009
Page: [56 - 62]
Pages: 7
DOI: 10.2174/157018009787158472

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