Synthesis and Biological Evaluation of a Biotinylated Paclitaxel with an Extra-Long Chain Spacer Arm

被引：19

作者：

Lis, Lev. G. ^{[1
,2
]}

Smart, Mary A. ^{[1
,2
]}

Luchniak, Anna ^{[3
]}

Gupta, Mohan L., Jr. ^{[3
]}

Gurvich, Vadim J. ^{[1
,2
]}

机构：

[1] Univ Minnesota, Inst Therapeut Discovery & Dev, Minneapolis, MN 55414 USA

[2] Univ Minnesota, Dept Med Chem, Minneapolis, MN 55414 USA

[3] Univ Chicago, Dept Mol Genet & Cell Biol, Chicago, IL 60637 USA

来源：

ACS MEDICINAL CHEMISTRY LETTERS | 2012年 / 3卷 / 09期

基金：

美国国家卫生研究院;

关键词：

paclitaxel; taxol; biotin; biotinylated; ANTICANCER AGENTS; ANTITUMOR AGENTS; OVARIAN-CANCER; INTRACELLULAR DELIVERY; PAMAM DENDRIMERS; NATURAL-PRODUCTS; TAXOL; FLUORESCENT; CHEMISTRY; MECHANISM;

D O I：

10.1021/ml300149z

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A biotinylated paclitaxel derivative with an extra-long chain (LC-LC-biotin) spacer arm was synthesized using an improved synthetic reaction sequence. The biotinylated paclitaxel analogue retained excellent microtubule stabilizing activity in vitro. Furthermore, it was shown that this analogue can simultaneously engage streptavidin and the binding site on microtubules, making it suitable for localization studies or for the attachment of paclitaxel to solid substrates via a streptavidin linkage.

引用

页码：745 / 748

页数：4

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