Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1395319 | European Journal of Medicinal Chemistry | 2009 | 9 Pages |
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.
Graphical abstractA series of new dipyrrolo- and furopyrrolopyrazinones related to cytotoxic tripentones were synthesized and evaluated as potential (CDKs1–5, GSK-3) kinase inhibitors.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Christophe Rochais, Nghia Vu Duc, Elodie Lescot, Jana Sopkova-de Oliveira Santos, Ronan Bureau, Laurent Meijer, Patrick Dallemagne, Sylvain Rault,