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新型紫草素类似物的合成与生物活性。

Synthesis and biological activity of novel shikonin analogues.

机构信息

Department of Medicinal Chemistry, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, PR China.

出版信息

Bioorg Med Chem Lett. 2009 Feb 1;19(3):735-7. doi: 10.1016/j.bmcl.2008.12.032. Epub 2008 Dec 11.

Abstract

A series of shikonin analogues with side chain variants have been synthesized and evaluated for antitumor activity. These novel analogues show a broad spectrum of in vitro cytotoxicity against various cancer cell lines. Additionally, some analogues were also found to have the ability to decrease the expression level of HIF-1alpha in breast cancer cells MDA-MB-231 under hypoxia. The features of these analogues suggest their potential in cancer therapy.

摘要

已经合成了一系列具有侧链变体的紫草素类似物,并对其抗肿瘤活性进行了评估。这些新型类似物对各种癌细胞系表现出广泛的体外细胞毒性。此外,还发现一些类似物在缺氧条件下能够降低乳腺癌细胞 MDA-MB-231 中 HIF-1alpha 的表达水平。这些类似物的特点表明它们在癌症治疗中的潜力。

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