New scaffolds for the design of selective estrogen receptor modulators Academic Article uri icon

Overview

MeSH Major

  • Drug Design
  • Selective Estrogen Receptor Modulators

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.

publication date

  • September 30, 2008

Research

keywords

  • Academic Article

Identity

Language

  • eng

Digital Object Identifier (DOI)

  • 10.1039/b806918b

PubMed ID

  • 19082149

Additional Document Info

start page

  • 3486

end page

  • 96

volume

  • 6

number

  • 19