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

doi:10.1016/j.bmc.2003.12.003

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

Pharmacology

Research output: Contribution to journal › Article

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 language	English (US)
Pages (from-to)	1029-1036
Number of pages	8
Journal	Bioorganic and Medicinal Chemistry
Volume	12
Issue number	5
DOIs	https://doi.org/10.1016/j.bmc.2003.12.003
Publication status	Published - 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

Cite this

Gorczynski, M. J., Leal, R. M., Mooberry, S. L., Bushweller, J. H., & Brown, M. L. (2004). Synthesis and evaluation of substituted 4-aryloxy- and 4-arylsulfanyl- phenyl-2-aminothiazoles as inhibitors of human breast cancer cell proliferation. Bioorganic and Medicinal Chemistry, 12(5), 1029-1036. https://doi.org/10.1016/j.bmc.2003.12.003

Synthesis and evaluation of substituted 4-aryloxy- and 4-arylsulfanyl- phenyl-2-aminothiazoles as inhibitors of human breast cancer cell proliferation. / Gorczynski, Michael J.; Leal, Rachel M.; Mooberry, Susan L.; Bushweller, John H.; Brown, Milton L.

In: Bioorganic and Medicinal Chemistry, Vol. 12, No. 5, 01.03.2004, p. 1029-1036.

Research output: Contribution to journal › Article

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10.1016/j.bmc.2003.12.003