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Elsevier, European Journal of Medicinal Chemistry, 2(44), p. 708-716

DOI: 10.1016/j.ejmech.2008.05.011

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Synthesis of new dipyrrolo- and furopyrrolopyrazinones related to tripentones and their biological evaluation as potential kinases (CDKs1-5, GSK-3) inhibitors.

Journal article published in 2008 by Christophe Rochais, Nghia Vu Duc, Elodie Lescot, Jana Sopkova-De Oliveira Santos, Ronan Bureau, Laurent Meijer, Patrick Dallemagne ORCID, Sylvain Rault
This paper was not found in any repository, but could be made available legally by the author.
This paper was not found in any repository, but could be made available legally by the author.

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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.