On March 1, 1996, 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. published an article.Recommanded Product: 29704-38-9 The title of the article was New Mustard Prodrugs for Antibody-Directed Enzyme Prodrug Therapy: Alternatives to the Amide Link. And the article contained the following:
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 I (R = MeSO3, X = CO), currently on clin. trial is a benzamide and is cleaved by CPG2 to a benzoic acid mustard drug II (R1 = CO2H). The authors have synthesized a series of new prodrugs I (R = Cl, X = O2C, NHCO, CH2CO, SCO, COS, CH2CS) where the benzamide link has been replaced by, for example, carbamate or ureido. Some of these alternative links are good substrates for CPG2 and therefore new candidates for ADEPT. The active drugs II (R = Cl, R1 = OH, NH2), derived from the best of these prodrugs are potent cytotoxic agents (1-2 μM) some 100 times more than I( R= MeSO3, R1 = CO2H). The prodrugs I (R = Cl, X = O2C, NHCO) are some 100-200-fold less cytotoxic, in a proliferating cell assay, than their corresponding active drugs II. The experimental process involved the reaction of tert-Butyl 2-(4-nitrophenyl)acetate(cas: 29704-38-9).Recommanded Product: 29704-38-9
The Article related to glutamate mustard prodrug preparation cytotoxicity, antibody directed enzyme prodrug therapy substrate, Amino Acids, Peptides, and Proteins: Amino Acids and other aspects.Recommanded Product: 29704-38-9
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics