Abstract

A series of (5Z)-5-ylidene-thiazolidine-4-one derivatives bearing the N-(4,5-dihalogenopyrrol-2-yl)carbamoyl fragment of Dispacamide A was prepared through a newly developed approach using a solution phase protocol assisted by microwave irradiation. These new compounds were synthesized in good yields (10-98%) by sulphur/nitrogen displacement or eventually by Knoevenagel condensation in the presence of a base (AcONa) in AcOH solution. The ten synthetic products have been obtained with a Z-geometry about their exocyclic double bond. All these compounds have been evaluated against eight protein kinases and human cell lines.

Keywords: Cell line, Dispacamide A, 2-imino-thiazolidine-4-one, inhibition, Knoevenagel reaction, microwave, solution phase, thiazolidine-4-one, sulphur/nitrogen displacement, protein kinase.