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.
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页码：1761 / 1766
页数：6
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