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.
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 (IC(50) = 0.041 μM).
authors.affiliation: 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. ; Université d'Abobo-Adjamé, Laboratoire de Chimie Bioorganique et de Subtances Naturelles (LCBSN), BP 802, Abidjan 02, République de la Côte d'Ivoire.
authors.forename: Wacothon Karime
authors.initials: WK
authors.lastname: Coulibaly
authors.forename: Ludovic
authors.initials: L
authors.lastname: Paquin
authors.forename: Anoubilé
authors.initials: A
authors.lastname: Bénié
authors.forename: Yves-Alain
authors.initials: YA
authors.lastname: Bekro
authors.forename: Emilie
authors.initials: E
authors.lastname: Durieux
authors.forename: Laurent
authors.initials: L
authors.lastname: Meijer
authors.forename: Rémy
authors.initials: R
authors.lastname: Le Guével
authors.forename: Anne
authors.initials: A
authors.lastname: Corlu
authors.forename: Jean-Pierre
authors.initials: JP
authors.lastname: Bazureau