Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
Email: lddd@benthamscience.org


Synthesis of Nimesulide Based New Class of Succinimide Analogues: Their Evaluation as Potential Cytotoxic Agents

Author(s): Kavitha Kankanala, Vangala Ranga Reddy, Yumnam Priyadarshini Devi, Lakshmi Narasu Mangamoori, Khagga Mukkanti, Sarbani Pal.


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

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Article Details

Year: 2012
Page: [742 - 748]
Pages: 7
DOI: 10.2174/157018012802652921
Price: $58