2. Academic Validation
  3. Synthesis and biological evaluation of novel thio-substituted chromanes as high-affinity partial agonists for the estrogen receptor

Synthesis and biological evaluation of novel thio-substituted chromanes as high-affinity partial agonists for the estrogen receptor

  • Bioorg Med Chem Lett. 2002 Jan 7;12(1):17-9. doi: 10.1016/s0960-894x(01)00679-5.
Lise B Christiansen 1,  Martin Wenckens,  Paul S Bury,  Birgitte Gissel,  Birgit S Hansen,  Susan M Thorpe,  Poul Jacobsen,  Anders Kanstrup,  Anker S Jørgensen,  Lars Naerum,  Karsten Wassermann
Affiliations

Affiliation

  • 1 Health Care Discovery & Preclinical Development, Novo Nordisk A/S, Novo Nordisk Park, DK-2760, Måløv, Denmark. libc@novonordisk.com
PMID: 11738564 DOI: 10.1016/s0960-894x(01)00679-5
Abstract

Synthesis of (+/-)-cis-7-hydroxy-3-phenyl-4-(4-(2-piperidinoethanethio)phenyl)chromane (13) and (+/-)-cis-7-hydroxy-3-phenyl-4-(4-(2-pyrrolidinoethanethio)phenyl)chromane (15) is presented. These compounds are representatives of a novel class of compounds with high in vitro binding affinity for the Estrogen receptor (IC(50)=7-10 nM), and very low in vitro uterotrophic activity (max stim.=5-17% rel to moxestrol; EC(50)=0.5-1.8 nM).

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