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用于黑色素瘤的噻唑烷类似物的合成及其抗增殖活性

Synthesis and antiproliferative activity of thiazolidine analogs for melanoma.

作者信息

Li Wei, Lu Yan, Wang Zhao, Dalton James T, Miller Duane D

机构信息

Department of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, Memphis, TN 38163, USA.

出版信息

Bioorg Med Chem Lett. 2007 Aug 1;17(15):4113-7. doi: 10.1016/j.bmcl.2007.05.059. Epub 2007 May 23.

Abstract

We have previously described 2-aryl-thiazolidine-4-carboxylic acid amides as a novel class of antiproliferative agents for prostate cancer. Screening these compounds with melanoma cell lines revealed that several of them have potent antiproliferative activity and selectivity against melanoma. To further improve the potency and selectivity, we synthesized a new series of analogs and tested them in two melanoma cell lines and fibroblast cells (negative controls). Comparison of anticancer effects of these compounds with a standard chemotherapeutic agent, sorafenib, showed that they are very effective in killing melanoma cells with low micromolar to nanomolar antiproliferative activity and provide us a new lead for developing potential drugs for melanoma.

摘要

我们之前已将2-芳基噻唑烷-4-羧酸酰胺描述为一类新型的前列腺癌抗增殖剂。用黑色素瘤细胞系筛选这些化合物后发现,其中几种对黑色素瘤具有强效的抗增殖活性和选择性。为了进一步提高效力和选择性,我们合成了一系列新的类似物,并在两种黑色素瘤细胞系和成纤维细胞(阴性对照)中对其进行了测试。将这些化合物的抗癌效果与标准化疗药物索拉非尼进行比较,结果表明它们在杀死黑色素瘤细胞方面非常有效,具有低微摩尔至纳摩尔的抗增殖活性,为我们开发潜在的黑色素瘤药物提供了新的线索。

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