Synthesis and antiproliferative activity of imidazole and imidazoline analogs for melanoma

Jianjun Chen, Zhao Wang, Yan Lu, James T. Dalton, Duane Miller, Wei Li

Research output: Contribution to journalArticle

37 Citations (Scopus)

Abstract

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.

Original languageEnglish (US)
Pages (from-to)3183-3187
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume18
Issue number11
DOIs
StatePublished - Jun 1 2008

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Thiazolidines
Imidazolines
Melanoma
Cells
Fibroblasts
Amides
Cell Line
imidazole

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

Cite this

Synthesis and antiproliferative activity of imidazole and imidazoline analogs for melanoma. / Chen, Jianjun; Wang, Zhao; Lu, Yan; Dalton, James T.; Miller, Duane; Li, Wei.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 18, No. 11, 01.06.2008, p. 3183-3187.

Research output: Contribution to journalArticle

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