Synthesis and Biological Evaluation of Pretubulysin and Derivatives

被引：73
|
作者：
Ullrich, Angelika [1 ]
Herrmann, Jennifer [2 ]
Mueller, Rolf [2 ]
Kazmaier, Uli [1 ]
机构：
[1] Univ Saarland, Inst Organ Chem, D-66041 Saarbrucken, Germany
[2] Univ Saarland, Dept Pharmaceut Biotechnol, D-66041 Saarbrucken, Germany
来源：
EUROPEAN JOURNAL OF ORGANIC CHEMISTRY | 2009年 / 2009卷 / 36期
关键词：
Total synthesis; Antitumor agents; Myxobacteria; Natural products; Tubulysins; Pretubulysin; AMINO-ACIDS; TUBULYSIN ANALOGS; MYXOBACTERIA; PEPTIDES; CONSTITUENTS; ANTICANCER; CRYSTAL;
D O I：
10.1002/ejoc.200900999
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
Pretubulysin, a biosynthetic precursor of the tubulysins, shows potent biological activity in the subnanomolar range towards various tumor cell lines. Its activity is only slightly less than those of the structurally more complex tubulysins. With a straightforward synthesis to hand, pretubulysin is an ideal lead structure for the development of tubulysin-based anticancer drugs ((C) Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2009)
引用
收藏
页码：6367 / 6378
页数：12
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