Structure-activity relationships for a family of benzothiophene selective estrogen receptor modulators including raloxifene and arzoxifene

Cassia R. Overk, Kuan Wei Peng, Rezene T. Asghodom, Irida Kastrati, Daniel D. Lantvit, Zhihui Qin, Jonna Frasor, Judy L. Bolton, Gregory R.J. Thatcher

Research output: Contribution to journalArticlepeer-review

35 Scopus citations

Abstract

The search for the "ideal" selective estrogen receptor modulator (SERM) as a substitute for hormone replacement therapy (HRT) or use in cancer chemoprevention has focused on optimization of estrogen receptor (ER) ligand binding. Based on the clinical and preclinical benzothiophene SERMs, raloxifene and arzoxifene, a family of SERMs has been developed to modulate activity and oxidative lability. Antiestrogenic potency measured in human endometrial and breast cancer cells, and ER ligand binding data were correlated and seen to provide a guide to SERM design only when viewed in toto. The in vitro studies were extended to the juvenile rat model, in which the desired antiestrogenic profile and putative cardiovascular benefits of SERMs were observed.

Original languageEnglish (US)
Pages (from-to)1520-1526
Number of pages7
JournalChemMedChem
Volume2
Issue number10
DOIs
StatePublished - Oct 8 2007
Externally publishedYes

Keywords

  • Cancer
  • Chemoprevention
  • Estradiol
  • Estrogen receptor
  • Hormone replacement therapy
  • SERM

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Pharmacology
  • Drug Discovery
  • Pharmacology, Toxicology and Pharmaceutics(all)
  • Organic Chemistry

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