Format

Send to

Choose Destination
Org Biomol Chem. 2008 Oct 7;6(19):3486-96. doi: 10.1039/b806918b. Epub 2008 Aug 4.

New scaffolds for the design of selective estrogen receptor modulators.

Author information

1
Departamento de Química, Facultad de Farmacia, Universidad San Pablo CEU, 28668-Boadilla del Monte, Madrid, Spain.

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.

PMID:
19082149
DOI:
10.1039/b806918b
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for Royal Society of Chemistry
Loading ...
Support Center