PMID- 14980616 OWN - NLM STAT- MEDLINE DCOM- 20041015 LR - 20220321 IS - 0968-0896 (Print) IS - 0968-0896 (Linking) VI - 12 IP - 5 DP - 2004 Mar 1 TI - Synthesis and evaluation of substituted 4-aryloxy- and 4-arylsulfanyl-phenyl-2-aminothiazoles as inhibitors of human breast cancer cell proliferation. PG - 1029-36 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 (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. FAU - Gorczynski, Michael J AU - Gorczynski MJ AD - Department of Chemistry, University of Virginia, Charlottesville, VA 22904, USA. FAU - Leal, Rachel M AU - Leal RM FAU - Mooberry, Susan L AU - Mooberry SL FAU - Bushweller, John H AU - Bushweller JH FAU - Brown, Milton L AU - Brown ML LA - eng PT - Journal Article PT - Research Support, Non-U.S. Gov't PL - England TA - Bioorg Med Chem JT - Bioorganic & medicinal chemistry JID - 9413298 RN - 0 (Estrogens) RN - 0 (Thiazoles) RN - 80168379AG (Doxorubicin) SB - IM MH - Breast Neoplasms/*pathology MH - Cell Division/drug effects MH - Cell Line, Tumor MH - Doxorubicin MH - Drug Resistance, Neoplasm MH - Estrogens/analysis MH - Female MH - Humans MH - Inhibitory Concentration 50 MH - Structure-Activity Relationship MH - Thiazoles/*chemical synthesis/*pharmacology EDAT- 2004/02/26 05:00 MHDA- 2004/10/16 09:00 CRDT- 2004/02/26 05:00 PHST- 2003/08/22 00:00 [received] PHST- 2003/11/25 00:00 [revised] PHST- 2003/12/10 00:00 [accepted] PHST- 2004/02/26 05:00 [pubmed] PHST- 2004/10/16 09:00 [medline] PHST- 2004/02/26 05:00 [entrez] AID - S0968089603008514 [pii] AID - 10.1016/j.bmc.2003.12.003 [doi] PST - ppublish SO - Bioorg Med Chem. 2004 Mar 1;12(5):1029-36. doi: 10.1016/j.bmc.2003.12.003.