抗肿瘤药337. 多拉司他汀10结构修饰的合成。
Antineoplastic agents 337. Synthesis of dolastatin 10 structural modifications.
作者信息
Pettit G R, Srirangam J K, Barkoczy J, Williams M D, Durkin K P, Boyd M R, Bai R, Hamel E, Schmidt J M, Chapuis J C
机构信息
Cancer Research Institute, Arizona State University, Tempe 85287-16-4, USA.
出版信息
Anticancer Drug Des. 1995 Oct;10(7):529-44.
New structural modifications of the marine shell-less mollusk peptide constituent dolastatin 10 (1) have been synthesized, and evaluated against a variety of cancer cell lines and for their ability to inhibit tubulin polymerization. A number of useful structure-activity relationships were uncovered. The most important observation was that the dolaphenine unit of dolastatin 10 could be satisfactorily replaced with a phenethylamine. Peptide 11C, designated auristatin PE, was found to exhibit inhibition of cancer cell growth and tubulin assembly comparable to that of dolastatin 10.
已合成了海洋无壳软体动物肽成分多拉司他汀10（1）的新结构修饰物，并针对多种癌细胞系对其进行了评估，还评估了它们抑制微管蛋白聚合的能力。发现了许多有用的构效关系。最重要的观察结果是，多拉司他汀10的多拉芬宁单元可以令人满意地被苯乙胺取代。发现肽11C（命名为奥瑞他汀PE）对癌细胞生长和微管蛋白组装的抑制作用与多拉司他汀10相当。
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