Letters in Drug Design & Discovery

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

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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.

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

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Article Details

VOLUME: 9
ISSUE: 8
Year: 2012
Page: [742 - 748]
Pages: 7
DOI: 10.2174/157018012802652921
Price: $58