Document Detail

2-phenyl-1-[4-(2-piperidine-1-yl-ethoxy)benzyl]-1H-benzimidazoles as ligands for the estrogen receptor: synthesis and pharmacological evaluation.
MedLine Citation:
PMID:  20598555     Owner:  NLM     Status:  MEDLINE    
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.
Sandra Dettmann; Katrin Szymanowitz; Anja Wellner; Anke Schiedel; Christa E Müller; Ronald Gust
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Publication Detail:
Type:  Journal Article     Date:  2010-06-09
Journal Detail:
Title:  Bioorganic & medicinal chemistry     Volume:  18     ISSN:  1464-3391     ISO Abbreviation:  Bioorg. Med. Chem.     Publication Date:  2010 Jul 
Date Detail:
Created Date:  2010-07-13     Completed Date:  2010-11-23     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9413298     Medline TA:  Bioorg Med Chem     Country:  England    
Other Details:
Languages:  eng     Pagination:  4905-16     Citation Subset:  IM    
Copyright Information:
Copyright (c) 2010. Published by Elsevier Ltd.
Institut für Pharmazie, Freie Universität Berlin, Königin-Luise-Str. 2+4, D-14195 Berlin, Germany.
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MeSH Terms
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
Gene Expression Regulation, Neoplastic / drug effects*
Reg. No./Substance:
0/Antineoplastic Agents; 0/Benzimidazoles; 0/Estrogen Receptor beta

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