Design, synthesis, and biological evaluation of novel water-soluble N-mustards as potential anticancer agents

N Kapuriya, R Kakadiya, H Dong, A Kumar…

Index: Kapuriya, Naval; Kakadiya, Rajesh; Dong, Huajin; Kumar, Amit; Lee, Pei-Chih; Zhang, Xiuguo; Chou, Ting-Chao; Lee, Te-Chang; Chen, Ching-Huang; Lam, King; Marvania, Bhavin; Shah, Anamik; Su, Tsann-Long Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 1 p. 471 - 485

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Citation Number: 23

Abstract

A series of novel water-soluble N-mustard-benzene conjugates bearing a urea linker were synthesized. The benzene moiety contains various hydrophilic side chains are linked to the meta-or para-position of the urea linker via a carboxamide or an ether linkage. The preliminary antitumor studies revealed that these agents exhibited potent cytotoxicity in vitro and therapeutic efficacy against human tumor xenografts in vivo. Remarkably, complete ...