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

Research output: Contribution to journal › Article › peer-review

55 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
State	Published - Mar 1 2004
Externally published	Yes

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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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 › peer-review

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AU - Brown, Milton L.

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AB - 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.

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