Synthesis and antitumor activity of water-soluble duocarmycin B1 prodrugs

Bioorganic & Medicinal Chemistry Letters
1999.0

Abstract

The water-soluble duocarmycin B1 prodrugs such as glycoside 3, phosphate 4 and carbamate 5 were synthesized for improving biological and pharmaceutical profiles of duocarmycin. Among these prodrugs, N-methylpiperazinylcarbamoyl derivative 5 exhibited potent antitumor activity against several human tumors in vivo.

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