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Lead identification of a potent benzopyranone selective estrogen receptor modulator
- Source :
- Bioorganicmedicinal chemistry letters. 14(13)
- Publication Year :
- 2002
-
Abstract
- Starting from a phenol screening hit (6), three series of benzopyranone selective estrogen receptor modulators (SERMs) have been designed, synthesized, and analyzed for both estrogen receptor alpha binding affinity and in vitro activity in two cell assays. The lead compound identified, SP500263 (13), was more potent than raloxifene and tamoxifen in a cell-based assay measuring inhibition of interleukin-6 release.
- Subjects :
- Clinical Biochemistry
Cell
Pharmaceutical Science
Pharmacology
Biochemistry
chemistry.chemical_compound
Estrogen Receptor Modulators
Piperidines
Coumarins
Drug Discovery
medicine
Tumor Cells, Cultured
Animals
Raloxifene
Molecular Biology
Binding Sites
Estradiol
Molecular Structure
Chemistry
Interleukin-6
Organic Chemistry
Estrogen Antagonists
Estrogen Receptor alpha
Ligand (biochemistry)
In vitro
Tamoxifen
medicine.anatomical_structure
Selective estrogen receptor modulator
Raloxifene Hydrochloride
Molecular Medicine
Female
Estrogen receptor alpha
Lead compound
hormones, hormone substitutes, and hormone antagonists
medicine.drug
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 14
- Issue :
- 13
- Database :
- OpenAIRE
- Journal :
- Bioorganicmedicinal chemistry letters
- Accession number :
- edsair.doi.dedup.....5671bfae4e2deb683ad3fb739f4caaed