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Synthesis and antitumor activity of water-soluble duocarmycin B1 prodrugs
A Asai1, S Nagamura, E Kobayashi
1Tokyo Research Laboratories, Kyowa Hakko Kogyo Co., Japan.
Bioorganic & Medicinal Chemistry Letters
|November 26, 1999
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.