Antimitotic antitumor agents: synthesis, structure-activity relationships, and biological characterization of N-aryl-N'-(2-chloroethyl) ureas as new selective alkylating …

…, J Legault, J Lacroix, R C-Gaudreault

Index: Mounetou; Legault; Lacroix; C-Gaudreault Journal of Medicinal Chemistry, 2001 , vol. 44, # 5 p. 694 - 702

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Citation Number: 69

Abstract

A series of N-aryl-N'-(2-chloroethyl) ureas (CEUs) and derivatives were synthesized and evaluated for antiproliferative activity against a wide panel of tumor cell lines. Systematic structure-activity relationship (SAR) studies indicated that:(i) a branched alkyl chain or a halogen at the 4-position of the phenyl ring or a fluorenyl/indanyl group,(ii) an exocyclic urea function, and (iii) a N'-2-chloroethyl moiety were required to ensure significant cytotoxicity. ...