4'-Hydroxynorendoxifen

4'-Hydroxynorendoxifen is a synthetic, nonsteroidal antiestrogen of the triphenylethylene group.[1][2] It is a dual selective estrogen receptor modulator (SERM) and aromatase inhibitor (AI), and was derived from tamoxifen, a SERM, and norendoxifen, a metabolite of tamoxifen that has been found to act as an AI.[1][2] The drug has been suggested for potential development as a treatment for estrogen receptor (ER)-positive breast cancer.[1][2] It was synthesized in 2015.[1]

4'-Hydroxynorendoxifen
Clinical data
Other namesN,N-Didesmethyl-4,4'-dihydroxytamoxifen
Identifiers
IUPAC name
  • 4,4'-(1-(4-(2-Aminoethoxy)phenyl)but-1-ene-1,2-diyl)diphenol
ChemSpider
Chemical and physical data
FormulaC24H25NO3
Molar mass375.468 g·mol−1
3D model (JSmol)
SMILES
  • CCC(=C(C1=CC=C(O)C=C1)C1=CC=C(OCCN)C=C1)C1=CC=C(O)C=C1
InChI
  • InChI=1S/C24H25NO3/c1-2-23(17-3-9-20(26)10-4-17)24(18-5-11-21(27)12-6-18)19-7-13-22(14-8-19)28-16-15-25/h3-14,26-27H,2,15-16,25H2,1H3
  • Key:VYSGWFCGFKTGQC-UHFFFAOYSA-N

References
  1. Lv W, Liu J, Skaar TC, Flockhart DA, Cushman M (March 2015). "Design and synthesis of norendoxifen analogues with dual aromatase inhibitory and estrogen receptor modulatory activities". Journal of Medicinal Chemistry. 58 (6): 2623–48. doi:10.1021/jm501218e. PMC 4687028. PMID 25751283.
  2. Nagini S (2017). "Breast Cancer: Current Molecular Therapeutic Targets and New Players". Anti-Cancer Agents in Medicinal Chemistry. 17 (2): 152–163. doi:10.2174/1871520616666160502122724. PMID 27137076.
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