A new prodrug of paclitaxel: synthesis of Protaxel

被引：32

作者：

Seligson, AL ^{[1
]}

Terry, RC ^{[1
]}

Bressi, JC ^{[1
]}

Douglass, JG ^{[1
]}

Sovak, M ^{[1
]}

机构：

[1] Biophysica, La Jolla, CA 92037 USA

来源：

ANTI-CANCER DRUGS | 2001年 / 12卷 / 04期

关键词：

cancer; derivative; paclitaxel; prodrug; Protaxel; Taxol;

D O I：

10.1097/00001813-200104000-00002

中图分类号：

R73 [肿瘤学];

学科分类号：

100214 ;

摘要：

2' end 7 Polyol carbonates of paclitaxel were synthesized and screened as potential paclitaxel prodrugs, Paclitaxel is released from 7-(2 " ,3 " -dihydroxypropylcarbonato) paclitaxel (Protaxel) at rates inversely proportional to pH, by an intramolecular cyclization. Compared to paclitaxel, maximum tolerated i.v. or i.p. doses (MTD) of Protaxel are about 2.5- to 3-fold higher; its efficacy is substantially higher in human cancer line xenografts in athymic mice, especially in prostate PC-3, breast MDA-MB 468 and ovary OVCAR-1, [(C) 2001 Lippincott Williams & Wilkins.].

引用

页码：305 / 313

页数：9

共 38 条

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