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New scaffolds for the design of selective estrogen receptor modulators.
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- Additional Information
- Source:
Publisher: Royal Society of Chemistry Country of Publication: England NLM ID: 101154995 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1477-0539 (Electronic) Linking ISSN: 14770520 NLM ISO Abbreviation: Org Biomol Chem Subsets: MEDLINE
- Publication Information:
Original Publication: Cambridge, UK : Royal Society of Chemistry, c2003-
- Subject Terms:
- Abstract:
In the present work we report the synthesis of four new ER ligands which can be used as scaffolds for the introduction of the basic side chains necessary for antiestrogenic activity. Affinities and agonist/antagonist characterization of the ligands for both ERalpha and ERbeta have been determined in a competitive radioligand assay, and in an in vitro coactivator recruitment functional assay, respectively. Molecular modelling techniques have been used in order to rationalize the experimental results. Compound is reported as a novel ERbeta-agonist/ERalpha-antagonist. Two compounds show an interesting antitumour profile towards two pancreatic cancer cell lines and have been selected for in vivo assays.
- Accession Number:
0 (Estrogen Receptor alpha)
0 (Estrogen Receptor beta)
0 (Selective Estrogen Receptor Modulators)
4TI98Z838E (Estradiol)
- Publication Date:
Date Created: 20081217 Date Completed: 20090122 Latest Revision: 20131121
- Publication Date:
20231215
- Accession Number:
10.1039/b806918b
- Accession Number:
19082149
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