Structure-activity relationship studies of arylthiazolidine amides as selective cytotoxic agents for melanoma

Wei Li, Zhao Wang, Veeresa Gududuru, Blazej Zbytek, Andrzej T. Slominski, James T. Dalton, Duane Miller

Research output: Contribution to journalArticle

24 Citations (Scopus)

Abstract

New drugs are urgently needed for improved therapy for melanoma. Materials and Methods: Ninety-one novel compounds were evaluated in two melanoma and one normal skin cell lines to identify potential lead compounds with high potency and selectivity. Mechanisms of action for the best compound were also investigated. Results: Three potent lead structures (serine amino alcohols, serine amides and thiazolidines) were identified, with thiazolidines having both excellent potency and high selectivity when compared with sorafenib, a drug used extensively in clinical trials for melanoma. Analyzing the effect of the lead compound showed that it induced DNA degradation consistent with necrotic cell death. Conclusion: The lead structure represents a novel class of compounds that can be further optimized for potential drug to treat advanced melanoma.

Original languageEnglish (US)
Pages (from-to)883-888
Number of pages6
JournalAnticancer research
Volume27
Issue number2
StatePublished - Mar 1 2007

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Cytotoxins
Structure-Activity Relationship
Amides
Melanoma
Thiazolidines
Serine
Pharmaceutical Preparations
Amino Alcohols
Cell Death
Clinical Trials
Cell Line
Skin
Lead
DNA
Therapeutics

All Science Journal Classification (ASJC) codes

  • Oncology
  • Cancer Research

Cite this

Structure-activity relationship studies of arylthiazolidine amides as selective cytotoxic agents for melanoma. / Li, Wei; Wang, Zhao; Gududuru, Veeresa; Zbytek, Blazej; Slominski, Andrzej T.; Dalton, James T.; Miller, Duane.

In: Anticancer research, Vol. 27, No. 2, 01.03.2007, p. 883-888.

Research output: Contribution to journalArticle

Li, W, Wang, Z, Gududuru, V, Zbytek, B, Slominski, AT, Dalton, JT & Miller, D 2007, 'Structure-activity relationship studies of arylthiazolidine amides as selective cytotoxic agents for melanoma', Anticancer research, vol. 27, no. 2, pp. 883-888.
Li W, Wang Z, Gududuru V, Zbytek B, Slominski AT, Dalton JT et al. Structure-activity relationship studies of arylthiazolidine amides as selective cytotoxic agents for melanoma. Anticancer research. 2007 Mar 1;27(2):883-888.
Li, Wei ; Wang, Zhao ; Gududuru, Veeresa ; Zbytek, Blazej ; Slominski, Andrzej T. ; Dalton, James T. ; Miller, Duane. / Structure-activity relationship studies of arylthiazolidine amides as selective cytotoxic agents for melanoma. In: Anticancer research. 2007 ; Vol. 27, No. 2. pp. 883-888.
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