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

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

Volume: 6 Issue: 1

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

Affiliation:

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

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.

Cite this article as:

Sechi Mario, Derudas Marco, Dallocchio Roberto, Dessì Alessandro, Cosseddu Alessia and Paglietti Giuseppe, DNA Binders: 1. Evaluation of DNA-Interactive Ability, Design, and Synthesis of Novel Intercalating Agents, Letters in Drug Design & Discovery 2009; 6 (1) . https://dx.doi.org/10.2174/157018009787158472