New mustard prodrugs for antibody-directed enzyme prodrug therapy: alternatives to the amide link

…, TA Connors, DC Blakey, AB Mauger

Index: Dowell, Robert I.; Springer, Caroline J.; Davies, David H.; Hadley, Elizabeth M.; Burke, Philip J.; Boyle, F. Thomas; Melton, Roger G.; Connors, Thomas A.; Blakey, David C.; Mauger, Anthony B. Journal of Medicinal Chemistry, 1996 , vol. 39, # 5 p. 1100 - 1105

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Citation Number: 51

Abstract

Antibody-directed enzyme prodrug therapy (ADEPT) is a two-step approach for the treatment of cancer which seeks to generate a potent cytotoxic agent selectively at a tumor site. In this work described the cytotoxic agent is generated by the action of an enzyme CPG2 on a relatively nontoxic prodrug. The prodrug 1 currently on clinical trial is a benzamide and is cleaved by CPG2 to a benzoic acid mustard drug 1a. We have synthesized a series of ...