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6-表-网抑素的合成改进及其对携带MDA-MB231人乳腺癌异种移植瘤小鼠的抗肿瘤疗效

Improved synthesis of 6-epi-dictyostatin and antitumor efficacy in mice bearing MDA-MB231 human breast cancer xenografts.

作者信息

Eiseman Julie L, Bai Lihua, Jung Won-Hyuk, Moura-Letts Gustavo, Day Billy W, Curran Dennis P

机构信息

Department of Pharmacology & Chemical Biology and University of Pittsburgh Cancer Institute, G.27.b Research Pavilion, Hillman Cancer Center, 5117 Centre Avenue, Pittsburgh, Pennsylvania 15213-1862, USA.

出版信息

J Med Chem. 2008 Nov 13;51(21):6650-3. doi: 10.1021/jm800979v. Epub 2008 Oct 8.

DOI:10.1021/jm800979v
PMID:18839939
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2627582/
Abstract

Structure-activity studies centered on the naturally occurring antitumor agent dictyostatin have recently identified several highly active epimers and analogues. From these compounds, 6- epi-dictyostatin was selected for scaleup preparation and evaluation in animals. Here we describe a new total synthesis that produced more than 30 mg of 6- epi-dictyostatin. The compound was found to have potent antitumor activity in SCID mice bearing MDA-MB231 human breast cancer xenografts.

摘要

以天然存在的抗肿瘤药物双鞭甲藻素为中心的构效关系研究最近鉴定出了几种高活性的差向异构体和类似物。从这些化合物中，选择了6-表双鞭甲藻素进行放大制备及动物实验评估。在此，我们描述了一种新的全合成方法，该方法制备出了超过30毫克的6-表双鞭甲藻素。在携带MDA-MB231人乳腺癌异种移植瘤的SCID小鼠中发现该化合物具有强大的抗肿瘤活性。

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本文引用的文献

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