Tetrahedron

Design, synthesis and evaluation of imidazolylmethyl carbamate prodrugs of alkylating agents

MP Hay, WR Wilson, WA Denny

Index: Hay, Michael P.; Wilson, William R.; Denny, William A. Tetrahedron, 2000 , vol. 56, # 4 p. 645 - 657

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Citation Number: 38

Abstract

Two approaches to prodrugs of alkylating agents based on an imidazolylmethyl carbamate nucleus were explored. A 2-azido analogue (3) of the bis-carbamate carmethizole (1) displayed similar aerobic cytotoxicity to 1 in a panel of human and murine cell lines. Approaches to the 2-amino and 2-carbamoyl analogues are described. In the second approach an imidazolylmethanol was used as a 'trigger'linked via a carbamate to the ...