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Article

Synthesis of New N,N'-Bis(5-arylidene-4-oxo-4,5-dihydrothiazolin-2-yl)piperazine Derivatives Under Microwave Irradiation and Preliminary Biological Evaluation

by
Wacothon Karime COULIBALY
1,2,
Ludovic PAQUIN
1,
Anoubilé BÉNIÉ
2,
Yves-Alain BEKRO
2,
Emilie DURIEUX
3,
Laurent MEIJER
4,
Rémy LE GUÉVEL
5,
Anne CORLU
5 and
Jean-Pierre BAZUREAU
1,*
1
Université de Rennes 1, Institut des Sciences Chimiques de Rennes (ISCR), UMR CNRS 6226, groupe Ingénièrie Chimique et Molécules pour le Vivant (ICMV), Bât. 10A, campus de Beaulieu, Avenue du Général Leclerc, CS 74205, 35042 Rennes Cedex, France
2
Université d'Abobo-Adjamé, Laboratoire de Chimie Bioorganique et de Subtances Naturelles (LCBSN), BP 802, Abidjan 02, République de la Côte d'Ivoire
3
Protein Phosphorylation and Human Disease Group, Station Biologique CNRS, Place G. Tessier, BP 74, 29682 Roscoff, France
4
ManRos Therapeutics (From Sea to Pharmacy), Hôtel de Recherche, Centre de Perharidy, 29680 Roscoff, France
5
Université de Rennes 1, ImPACcell Platform, IFR 140, Bât. 8, 2 Avenue du Prof. Léon Bernard, CS 34317, 35043 Rennes Cedex, France
*
Author to whom correspondence should be addressed.
Sci. Pharm. 2012, 80(4), 825-836; https://doi.org/10.3797/scipharm.1206-04
Submission received: 4 June 2012 / Accepted: 16 September 2012 / Published: 16 September 2012
Versions Notes

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).
Keywords: 5-Arylidene rhodanine; 2,2'-(Piperazine-1,4-diyl)bis(5-benzylidene-1,3-thiazol-4(5H)-one); Microwave irradiation; Cytotoxity; Protein kinase; Diamines 5-Arylidene rhodanine; 2,2'-(Piperazine-1,4-diyl)bis(5-benzylidene-1,3-thiazol-4(5H)-one); Microwave irradiation; Cytotoxity; Protein kinase; Diamines

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MDPI and ACS Style

COULIBALY, W.K.; PAQUIN, L.; BÉNIÉ, A.; BEKRO, Y.-A.; DURIEUX, E.; MEIJER, L.; LE GUÉVEL, R.; CORLU, A.; BAZUREAU, J.-P. Synthesis of New N,N'-Bis(5-arylidene-4-oxo-4,5-dihydrothiazolin-2-yl)piperazine Derivatives Under Microwave Irradiation and Preliminary Biological Evaluation. Sci. Pharm. 2012, 80, 825-836. https://doi.org/10.3797/scipharm.1206-04

AMA Style

COULIBALY WK, PAQUIN L, BÉNIÉ A, BEKRO Y-A, DURIEUX E, MEIJER L, LE GUÉVEL R, CORLU A, BAZUREAU J-P. 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. 2012; 80(4):825-836. https://doi.org/10.3797/scipharm.1206-04

Chicago/Turabian Style

COULIBALY, Wacothon Karime, Ludovic PAQUIN, Anoubilé BÉNIÉ, Yves-Alain BEKRO, Emilie DURIEUX, Laurent MEIJER, Rémy LE GUÉVEL, Anne CORLU, and Jean-Pierre BAZUREAU. 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, no. 4: 825-836. https://doi.org/10.3797/scipharm.1206-04

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