No abstract

No abstract

International audienceA series of (5Z) 5-arylidene 2-thioxo-1,3-thiazolidin-4-one derivs. 7(a-l) bearing a [4-(3-aminopropyl)piperazin-1-yl]propyl side chain in N-3 position was prepd. using a soln. phase protocol assisted by microwave dielec. heating. These new compds. were synthesized in four steps with overall yields ranging from 12 to 33% via a "one-pot two-steps" protocol based on Holmberg reaction followed by a stereocontrolled Knoevenagel condensation. The rhodanine intermediate 4' issued from Holmberg reaction under microwave was also isolated and identified by spectroscopic methods of anal. The twelve deprotected products 7(a-l) have been obtained with a Z-geometry about their exocyclic double bond. All N-Boc intermediates 6(a-l) and deprotected rhodanine derivs. 7(a-l) issued from trifluoroacetic acid treatment have been characterized by 1H, 13C and HRMS

International audienceHerein, we report on the 5-step synthesis of new 3-[4-(arylalkoxy)phenylethyl]-2-thioxo-1,3-thiazolidin-4-ones without 5-arylidene fragments starting from tyramine The construction involved protection with Boc(2)O, regioselective O-alkylation, deprotection with 6 M HCl, neutralization, and finally reaction of bis(carboxymethyl) trithiocarbonate under microwave irradiation. The intermediates and the N-substituted rhodanine have been also evaluated for their in vitro inhibition of cell proliferation (Huh7, Caco 2, MDA-MB231, HCT 116, PC3, NCI-H727, HaCat). Two compounds have shown a selective potent activity against HCT116 cell line

Influence de la floraison sur la composition chimique et l'activité anti sinusite de l'huile essentielle des feuilles de Diphasia klaineana Pierre (Rutaceae) de Côte d'Ivoire