Microwave Assisted Organic Synthesis (MAOS) of New Dispacamide A Derivatives Bearing a Thiazolinone Platform, Biological Assays on Inhibition of Protein Kinases and Cell Effects

Author(s): Solene Guiheneuf, Ludovic Paquin, Francois Carreaux, Emilie Durieu, Helene Benedettid, Remy Le Guevel, Anne Corlu, Laurent Meijer, Jean-Pierre Bazureau

Journal Name: Current Microwave Chemistry

Volume 1 , Issue 1 , 2014

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Graphical Abstract:


A series of (5Z)-5-ylidene-thiazolidine-4-one derivatives bearing the N-(4,5-dihalogenopyrrol-2-yl)carbamoyl fragment of Dispacamide A was prepared through a newly developed approach using a solution phase protocol assisted by microwave irradiation. These new compounds were synthesized in good yields (10-98%) by sulphur/nitrogen displacement or eventually by Knoevenagel condensation in the presence of a base (AcONa) in AcOH solution. The ten synthetic products have been obtained with a Z-geometry about their exocyclic double bond. All these compounds have been evaluated against eight protein kinases and human cell lines.

Keywords: Cell line, Dispacamide A, 2-imino-thiazolidine-4-one, inhibition, Knoevenagel reaction, microwave, solution phase, thiazolidine-4-one, sulphur/nitrogen displacement, protein kinase.

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Article Details

Year: 2014
Published on: 26 August, 2013
Page: [33 - 40]
Pages: 8
DOI: 10.2174/22133356114019990002

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