Synthesis and antiproliferative activity of imidazole and imidazoline analogs for melanoma
作者:Jianjun Chen、Zhao Wang、Yan Lu、James T. Dalton、Duane D. Miller、Wei Li
DOI:10.1016/j.bmcl.2008.04.073
日期:2008.6
We have previously reported substituted 2-aryl-thiazolidine-4-carboxylic acid amides as potent and selective antiproliferative agents for melanoma. To understand the importance of the thiazolidine ring and to reduce potential complications associated with the two chiral centers, we designed and synthesized sets of new analogs by modifying this ring. These new analogs were tested in two melanoma cell
我们以前曾报道过取代的 2-芳基-噻唑烷-4-羧酸酰胺作为黑色素瘤的有效和选择性抗增殖剂。为了了解噻唑烷环的重要性并减少与两个手性中心相关的潜在并发症,我们通过修改该环设计并合成了多组新的类似物。这些新的类似物在两种黑色素瘤细胞系和成纤维细胞(阴性对照)中进行了测试。与含有噻唑烷环的旧类似物相比,这些新类似物总体上具有较低的效力,但其中一些类似物仍然具有非常好的选择性。这些结构-活性研究表明,噻唑烷环对于这些系列化合物的活性非常关键。