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Issue 19, 2008
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New scaffolds for the design of selective estrogen receptor modulators

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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 ERα and ERβ 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 2 is reported as a novel ERβ-agonist/ERα-antagonist. Two compounds show an interesting antitumour profile towards two pancreatic cancer cell lines and have been selected for in vivo assays.

Graphical abstract: New scaffolds for the design of selective estrogen receptor modulators

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Publication details

The article was received on 24 Apr 2008, accepted on 07 Jul 2008 and first published on 04 Aug 2008


Article type: Paper
DOI: 10.1039/B806918B
Citation: Org. Biomol. Chem., 2008,6, 3486-3496
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    New scaffolds for the design of selective estrogen receptor modulators

    S. Martín-Santamaría, J. Rodríguez, S. de Pascual-Teresa, S. Gordon, M. Bengtsson, I. Garrido-Laguna, B. Rubio-Viqueira, P. P. López-Casas, M. Hidalgo, B. de Pascual-Teresa and A. Ramos, Org. Biomol. Chem., 2008, 6, 3486
    DOI: 10.1039/B806918B

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