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:Farmaco Chimico Tossicologico, Universita di Sassari, Via Muroni 23/A, 07100 Sassari, Italy.
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.
