Synthesis of new N,N'-bis(5-arylidene-4-oxo- 4,5-dihydrothiazolin-2-yl)piperazine derivatives under microwave irradiation and preliminary biological evaluation

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Abstract

New N,N'-bis(5-arylidene-4-oxo-4,5-dihydrothiazoline-2-yl)diamine derivatives 5 were prepared in two steps from rhodanine and piperazine, or 1,4-bis(3-amino- propyl)piperazine, under microwave reaction conditions with retention of configuration. Some of these compounds were tested for in vitro antiproliferative activities and for their kinase inhibitory potencies towards six kinases (CDK5/p25, GSK3α/β, DYRK1A, DYRK2, CLK1, and CLK2). The compound 5d showed nanomolar activity towards DYRK1A kinase (IC50 = 0.041 μM)

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Coulibaly, W. K., Paquin, L., Bénié, A., Bekro, Y. A., Durieux, E., Meijer, L., … Bazureau, J. P. (2012). Synthesis of new N,N’-bis(5-arylidene-4-oxo- 4,5-dihydrothiazolin-2-yl)piperazine derivatives under microwave irradiation and preliminary biological evaluation. Scientia Pharmaceutica, 80(4), 825–836. https://doi.org/10.3797/scipharm.1206-04

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