ChemInform Abstract: A New Spacer Group Derived from Arylmalonaldehydes for Glucuronylated Prodrugs.

A new glucuronylated prodrug of doxorubicin, potentially useful for ADEPT or PMT cancer chemotherapy, has been prepared from 4-methyl phenyl malonaldehyde. The enol ether spacer, linked via a carbamate to the 3'-amino group of doxorubicin is rapidly cleaved after beta-glucuronidase (E coli) catalyzed hydrolysis at pH 7.2 and 37 degrees C. (C) 1998 Elsevier Science Ltd. All rights reserved.