SYNTHESIS AND ANTITUMOR EVALUATION OF PACLITAXEL PHOSPHONOOXYMETHYL ETHERS - A NOVEL CLASS OF WATER-SOLUBLE PACLITAXEL PRO-DRUGS

Authors
GOLIK J WONG HSL CHEN SH DOYLE TW WRIGHT JJK KNIPE J ROSE WC CASAZZA AM VYAS DM
Citation
J. Golik et al., SYNTHESIS AND ANTITUMOR EVALUATION OF PACLITAXEL PHOSPHONOOXYMETHYL ETHERS - A NOVEL CLASS OF WATER-SOLUBLE PACLITAXEL PRO-DRUGS, Bioorganic & medicinal chemistry letters, 6(15), 1996, pp. 1837-1842
Citations number
20
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
6
Issue
15
Year of publication
1996
Pages
1837 - 1842
Database
ISI
SICI code
0960-894X(1996)6:15<1837:SAAEOP>2.0.ZU;2-4
Abstract
The synthesis, pharmacokinetic properties, and antitumor evaluation of novel paclitaxel phosphonooxymethyl ether derivatives 8-11 and salts thereof is described. These compounds exhibit improved water solubilit y as compared to paclitaxel (1) and upon incubation with plasma and al kaline phosphatase they readily release parent drug. The in vivo antit umor evaluation of compounds 8-11 established them as suitable pro-dru gs of paclitaxel. Copyright (C) 1996 Elsevier Science Ltd