A straightforward click-approach towards pretubulysin-analogues

被引：14

作者：

Burkhart, Jens L. ^{[1
]}

Kazmaier, Uli ^{[1
]}

机构：

[1] Univ Saarland, Inst Organ Chem, D-66123 Saarbrucken, Germany

来源：

RSC ADVANCES | 2012年 / 2卷 / 09期

关键词：

METASTATIC BREAST-CANCER; ADVANCED SOLID TUMORS; DOLASTATIN; 10; ANGIOCOCCUS-DISCIFORMIS; BIOLOGICAL-PROPERTIES; POTENTIAL ANTICANCER; TUBULYSIN ANALOGS; PEPTIDE-SYNTHESIS; TUBULIN-BINDING; NATURAL-PRODUCT;

D O I：

10.1039/c2ra20191g

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

The [3+2]-cycloaddition of an azido tripeptide, corresponding to the left hand side of pretubulysin, with a range of alkynes, such as propiolic acid amides and propargyl ethers, allows the straightforward syntheses of libraries of tubulysin derivatives. Via this click approach, a chimera of pretubulysin and dolastatin 10, both highly potent antimitotic drug candidates, also becomes accessible.

引用

页码：3785 / 3790

页数：6

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