Synthesis and antitumor activity of water-soluble duocarmycin B1 prodrugs

Authors
Asai, A Nagamura, S Kobayashi, E Gomi, K Saito, H
Citation
A. Asai et al., Synthesis and antitumor activity of water-soluble duocarmycin B1 prodrugs, BIOORG MED, 9(20), 1999, pp. 2995-2998
Citations number
22
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
20
Year of publication
1999
Pages
2995 - 2998
Database
ISI
SICI code
0960-894X(19991018)9:20<2995:SAAAOW>2.0.ZU;2-6
Abstract
The water-soluble duocarmycin B1 prodrugs such as glycoside 3, phosphate 4 and carbamate 5 were synthesized for improving biological and pharmaceutica l profiles of duocarmycin. Among these prodrugs, N-methylpiperazinylcarbamo yl derivative 5 exhibited potent antitumor activity against several human t umors in vivo. (C) 1999 Elsevier Science Ltd. All rights reserved.