Doxorubicin prodrugs with reduced cytotoxicity suited for tumour-specific activation

Citation
S. Desbene et al., Doxorubicin prodrugs with reduced cytotoxicity suited for tumour-specific activation, ANTI-CAN DR, 13(8), 1998, pp. 955-968
Citations number
20
Categorie Soggetti
Onconogenesis & Cancer Research
Journal title
ANTI-CANCER DRUG DESIGN
ISSN journal
02669536 → ACNP
Volume
13
Issue
8
Year of publication
1998
Pages
955 - 968
Database
ISI
SICI code
0266-9536(199812)13:8<955:DPWRCS>2.0.ZU;2-O
Abstract
The three new hydrophilic prodrugs 2, 3 and 4 have been prepared from methy l (4-hydroxymethyl-2-nitrophenyl 2,3,4-tri-O-acetyl-beta-D-glucopyranosid)u ronate (5) and doxorubicin. Their low cytotoxicity, efficient release of do xorubicin after hydrolysis by beta-D-glucuronidase, and in the cases of 2 a nd 3 stability at pH 7.2 fulfil the preliminary requirement for their use i n antibody-directed enzyme prodrug therapy or prodrug monotherapy.