Synthesis of New Dipyrrolo- and Furopyrrolopyrazinones Related to Tripentones and Their Biological Evaluation As Potential Kinases (CDKs1-5, GSK-3) Inhibitors

Overview

Journal Eur J Med Chem

Specialty Chemistry

Date 2008 Jul 1

PMID 18586356

Citations 3

Authors

Christophe Rochais

Nghia Vu Duc

Elodie Lescot

Jana Sopkova-de Oliveira Santos

Ronan Bureau

Laurent Meijer

Patrick Dallemagne

Sylvain Rault

Affiliations

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Abstract

We herein describe the synthesis of novel dipyrrolo- and furopyrrolopyrazinones related to highly cytotoxic tripentones and to their oximes. The synthetic pathway involved in particular a Curtius rearrangement and a subsequent cyclisation into the title pyrazinones. The biological evaluation towards various cyclin-dependent kinases (CDKs1-5, GSK-3) highlighted a weak inhibitory activity for the oximes whose SAR was studied by a molecular modeling study.

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