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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

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 and Sarbani Pal

Volume 9, Issue 8, 2012

Page: [742 - 748] Pages: 7

DOI: 10.2174/157018012802652921

Price: $65

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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