Department of Medicinal Chemistry, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, PR China.
Bioorg Med Chem Lett. 2009 Feb 1;19(3):735-7. doi: 10.1016/j.bmcl.2008.12.032. Epub 2008 Dec 11.
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.
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。
