| 2-phenyl-1-[4-(2-piperidine-1-yl-ethoxy)benzyl]-1H-benzimidazoles as ligands for the estrogen receptor: synthesis and pharmacological evaluation. | |
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MedLine Citation:
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PMID: 20598555 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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2-phenyl-1H-benzimidazoles 7a-e were synthesized and tested for gene activation on ERalpha-positive MCF-7 breast cancer cells, stably transfected with the reporter plasmid EREwtcluc (MCF-7-2a cells). None of the compounds showed agonistic properties, but they antagonized dependent on hydroxyl groups at the benzimidazole core (5- or 6-OH) and at the aromatic ring in the 2-position (4-OH) in high concentrations the gene activation induced by estradiol (E2, 1 nM). All compounds exhibited significant antiproliferative properties on MCF-7 cells but they were inactive against hormone independent, ER negative MDA-MB-231 cells. |
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Authors:
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Sandra Dettmann; Katrin Szymanowitz; Anja Wellner; Anke Schiedel; Christa E Müller; Ronald Gust |
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Publication Detail:
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Type: Journal Article Date: 2010-06-09 |
Journal Detail:
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Title: Bioorganic & medicinal chemistry Volume: 18 ISSN: 1464-3391 ISO Abbreviation: Bioorg. Med. Chem. Publication Date: 2010 Jul |
Date Detail:
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Created Date: 2010-07-13 Completed Date: 2010-11-23 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 9413298 Medline TA: Bioorg Med Chem Country: England |
Other Details:
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Languages: eng Pagination: 4905-16 Citation Subset: IM |
Copyright Information:
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Copyright (c) 2010. Published by Elsevier Ltd. |
Affiliation:
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Institut für Pharmazie, Freie Universität Berlin, Königin-Luise-Str. 2+4, D-14195 Berlin, Germany. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Antineoplastic Agents
/
chemical synthesis,
chemistry*,
pharmacology* Benzimidazoles / chemical synthesis, chemistry*, pharmacology* Breast Neoplasms / drug therapy* Cell Line, Tumor Cell Proliferation / drug effects Estrogen Receptor beta / genetics*, metabolism Female Gene Expression Regulation, Neoplastic / drug effects* Humans |
| Chemical | |
Reg. No./Substance:
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0/Antineoplastic Agents; 0/Benzimidazoles; 0/Estrogen Receptor beta |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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