Novel prodrugs which are activated to cytotoxic alkylating agents by carboxypeptidase G2

CJ Springer, P Antoniw, F Searle…

Index: Springer, Caroline J.; Antoniw, Pari; Bagshawe, Kenneth D.; Searle, Frances; Bisset, Graham M. F.; Jarman, Michael Journal of Medicinal Chemistry, 1990 , vol. 33, # 2 p. 677 - 681

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Citation Number: 137

Abstract

The synthesis of three novel prodrugs, 4-[bis [2-(mesyloxy) ethyl] amino] benzoyl-1,-glutamic acid (7), 4-[(2-chloroethyl)[2-(mesyloxy) ethyl] amino] benzoyl-L-glutamic acid (8), and 44 bis (2-chloroethyl) amino] benzoyl-~ glutamic acid (9), for use as anticancer agents, is described here. Each is a bifunctional alkylating agent in which the activating effect of the ionized carboxyl function is masked through an amide bond to the glutamic acid residue. These ...