期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 18, 期 11, 页码 3183-3187出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.04.073
关键词
melanoma; thiazolidine; imidazole analogs; imidazoline analogs; structure-activity relationships
资金
- NCI NIH HHS [1R15CA125623-01A2, R15 CA125623, R15 CA125623-01A2] Funding Source: Medline
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.
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