Synthesis and evaluation of substituted 4-aryloxy- and 4-arylsulfanyl- phenyl-2-aminothiazoles as inhibitors of human breast cancer cell proliferation

Michael J. Gorczynski, Rachel M. Leal, Susan L. Mooberry, John H. Bushweller, Milton L. Brown

Research output: Contribution to journalArticle

53 Scopus citations

Abstract

Several substituted 4-aryloxy- and 4-arylsulfanyl-phenyl-2-aminothiazoles were synthesized and evaluated for cytotoxic activity against estrogen-positive, estrogen-negative, and adriamycin-resistant human breast cancer cell lines. 4-[4′-(3,4-Dichlorophenoxy)-phenyl]-thiazol-2-yl ammonium iodide demonstrated potent activity against both estrogen-positive and negative breast cancer cell lines with low micromolar (μM) GI50 values. In addition, we have identified several 2-aminothiazoles that demonstrated selective potency for the adriamycin-resistant and estrogen-negative breast cancer cell lines. The results suggest that these 2-aminothiazoles represent lead compounds for evaluation in animal models of breast cancer.

Original languageEnglish (US)
Pages (from-to)1029-1036
Number of pages8
JournalBioorganic and Medicinal Chemistry
Volume12
Issue number5
DOIs
Publication statusPublished - Mar 1 2004

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Keywords

  • 2-Aminothiazoles
  • Breast cancer
  • Diaryl ethers
  • Substituent effects

ASJC Scopus subject areas

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

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