Synthesis and antiproliferative activity of imidazole and imidazoline analogs for melanoma
Synthesis and antiproliferative activity of imidazole and imidazoline analogs for melanoma
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DOI：
10.1016/j.bmcl.2008.04.073
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发表时间：
2008-06-01
影响因子：
2.7
通讯作者：
Li, Wei
中科院分区：
文献类型：
--
作者：
Chen, Jianjun;Wang, Zhao;Li, Wei
我们以前报道过取代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，我们通过修饰该环设计并合成了一系列新的类似物。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，这些新类似物的效价一般较低，但其中一些类似物仍具有很好的选择性。这些结构活性研究表明，噻唑烷环对这些系列化合物的活性起着至关重要的作用。(C) 2008 Elsevier Ltd版权所有。
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 lines and fibroblast cells (negative controls). Compared with the older analogs containing the thiazolidine ring, these new analogs have lower potency in general, but some of these analogs still have very good selectivity. These structure-activity studies indicated that the thiazolidine ring is very critical for the activity for these series of compounds. (C) 2008 Elsevier Ltd. All rights reserved.