NOVEL WATER-SOLUBLE PHOSPHATE PRODRUGS OF TAXOL(R) POSSESSING IN-VIVOANTITUMOR-ACTIVITY

Authors
UEDA Y MIKKILINENI AB KNIPE JO ROSE WC CASAZZA AM VYAS DM
Citation
Y. Ueda et al., NOVEL WATER-SOLUBLE PHOSPHATE PRODRUGS OF TAXOL(R) POSSESSING IN-VIVOANTITUMOR-ACTIVITY, Bioorganic & medicinal chemistry letters, 3(8), 1993, pp. 1761-1766
Citations number
31
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
3
Issue
8
Year of publication
1993
Pages
1761 - 1766
Database
ISI
SICI code
0960-894X(1993)3:8<1761:NWPPOT>2.0.ZU;2-U
Abstract
Synthesis and biological evaluation of novel taxol derivatives having a phosphonoxyphenylpropionate ester group at the 2'-position or at the 7-position of taxol are described. These were found to have much impr oved water solubility and both were found to generate taxol upon expos ure to alkaline phosphatase. A particular derivative, 7-phosphonoxyphe nylpropionate of taxol 3b exhibited antitumor activity comparable to t hat of taxol against the ip/ip M109 murine tumor model.