Synthesis of New N,N'-Bis(5-arylidene-4-oxo-4,5-dihydrothiazolin-2-yl)piperazine Derivatives Under Microwave Irradiation and Preliminary Biological Evaluation. - Archive ouverte HAL Access content directly
Journal Articles Scientia Pharmaceutica Year : 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.

(1, 2) , (1) , (2) , (2) , (3) , (4) , (5) , (5) , (1)
1
2
3
4
5

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).
Fichier principal
Vignette du fichier
scipharm-2012-80-825.pdf (187 Ko) Télécharger le fichier
Origin : Publisher files allowed on an open archive
Loading...

Dates and versions

inserm-00864810 , version 1 (23-09-2013)

Identifiers

Cite

Wacothon Karime Coulibaly, Ludovic Paquin, Anoubilé Bénié, Yves-Alain Bekro, Emilie Durieux, et al.. 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), pp.825-36. ⟨10.3797/scipharm.1206-04⟩. ⟨inserm-00864810⟩
401 View
233 Download

Altmetric

Share

Gmail Facebook Twitter LinkedIn More