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- Title
Synthesis of New N,N'-Bis(5-arylidene-4-oxo- 4,5-dihydrothiazolin-2-yl)piperazine Derivatives Under Microwave Irradiation and Preliminary Biological Evaluation.
- Authors
COULIBALY, Wacothon Karime; PAQUIN, Ludovic; BÉNIÉ, Anoubilé; BEKRO, Yves-Alain; DURIEUX, Emilie; MEIJER, Laurent; LE GUÉVEL, Rémy; CORLU, Anne; BAZUREAU, Jean-Pierre
- 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).
- Subjects
PIPERAZINE; AZACONAZOLE; THIAZOLINES; KINASES; BIOCHEMISTRY
- Publication
Scientia Pharmaceutica, 2012, Vol 80, Issue 4, p825
- ISSN
0036-8709
- Publication type
Article
- DOI
10.3797/scipharm.1206-04