Abstract

Novel succinimide derivatives based on nimesulide were designed as potential anticancer agents and their synthesis was carried out using a straightforward and atom economic method. The key step of this methodology involved an Aza-Michael addition of several nitrogen nucleophiles to the corresponding N-aryl maleimide derivatives prepared efficiently from nimesulide via a two-step process. A number of compounds containing –NHX (X = Ar, NHCOR, NHAr etc) at the C-3 of the succinimide were prepared in good yields. A number of compounds synthesized were tested for their cytotoxicity in vitro against human colon cancer cell lines and some of them showed promising activities.

Keywords: Nimesulide, Succinimide, Aza-Michael addition, Cancer, cytotoxic activities, N-arylsuccinamic acids, cytotoxic succinimide derivatives, N-aryl maleimide, Doxorubicin, acylhydrazides