Synthesis and evaluation of substituted 4-aryloxy- and 4-arylsulfanyl-phenyl-2-aminothiazoles as inhibitors of human breast cancer cell proliferation.
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 (microM) GI(50) 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.
Department of Chemistry, University of Virginia, Charlottesville, VA 22904, USA.
Michael J
MJ
Gorczynski
Rachel M
RM
Leal
Susan L
SL
Mooberry
John H
JH
Bushweller
Milton L
ML
Brown
D001943:Breast Neoplasms / Q000473:pathology*; D002455:Cell Division / Q000187:drug effects; D045744:Cell Line, Tumor; D004317:Doxorubicin; D019008:Drug Resistance, Neoplasm; D004967:Estrogens / Q000032:analysis; D005260:Female; D006801:Humans; D020128:Inhibitory Concentration 50; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis* / Q000494:pharmacology*
D004967:Estrogens; D013844:Thiazoles; D004317:Doxorubicin