New scaffolds for the design of selective estrogen receptor modulators.


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.

DOI: 10.1039/b806918b

Cite this paper

@article{MartnSantamara2008NewSF, title={New scaffolds for the design of selective estrogen receptor modulators.}, author={Sonsoles Mart{\'i}n-Santamar{\'i}a and Jos{\'e}-Juan Rodr{\'i}guez and Sonia de Pascual-Teresa and Sandra Gordon and Martin Bengtsson and Ignacio Garrido-Laguna and Bel{\'e}n Rubio-Viqueira and Pedro Pablo L{\'o}pez-Casas and Manuel Hidalgo and Beatriz de Pascual-Teresa and Ana Raquel Xavier Ramos}, journal={Organic & biomolecular chemistry}, year={2008}, volume={6 19}, pages={3486-96} }