Synthesis and bioactivity of 2,4-diacyl analogues of paclitaxel

被引：16

作者：

Chordia, MD

Yuan, HQ

Jagtap, PG

Kadow, JF

Long, BH

Fairchild, CR

Johnston, KA

Kingston, DGI ^{[1
]}

机构：

[1] Virginia Polytech Inst & State Univ, Dept Chem, Blacksburg, VA 24061 USA

[2] Bristol Myers Squibb Co, Pharmaceut Res Inst, Wallingford, CT 06492 USA

[3] Bristol Myers Squibb Co, Pharmaceut Res Inst, Princeton, NJ USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2001年 / 9卷 / 01期

关键词：

D O I：

10.1016/S0968-0896(00)00233-9

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The 2,4-diacyl paclitaxel analogues 8a-8r were prepared from paclitaxel by acylation of 4-deacetyl-2-debenzoylpaclitaxel 1,2-carbonate (3) followed either by hydrolysis of the carbonate and acylation or by direct treatment of the carbonate with an aryllithium. Some of the resulting derivatives showed significantly improved tubulin assembly activity and cytotoxicity as compared with paclitaxel; in some cases this improvement was especially significant for paclitaxel-resistant cell lines. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：171 / 178

页数：8

共 34 条

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