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
收藏
页码：3785 / 3790
页数：6
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