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

被引：67

作者：

UEDA, Y

MIKKILINENI, AB

KNIPE, JO

ROSE, WC

CASAZZA, AM

VYAS, DM

机构：

[1] Pharmaceutical Research Institute, Bristol-Myers Squibb Company, Wallingford, CT 06492-7660

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1993年 / 3卷 / 08期

关键词：

D O I：

10.1016/S0960-894X(00)80058-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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 improved water solubility and both were found to generate taxol upon exposure to alkaline phosphatase. A particular derivative, 7-phosphonoxyphenylpropionate of taxol 3b exhibited antitumor activity comparable to that of taxol against the ip/ip M109 murine tumor model.

引用

页码：1761 / 1766

页数：6