Synthesis and pharmacological evaluation of novel cis-3,4-diaryl-hydroxychromanes as high affinity partial agonists for the estrogen receptor

  • Bioorg Med Chem. 2002 Jan;10(1):125-45. doi: 10.1016/s0968-0896(01)00257-7.
Paul S Bury  1 ,  Lise B Christiansen ,  Poul Jacobsen ,  Anker S Jørgensen ,  Anders Kanstrup ,  Lars Naerum ,  Steven Bain ,  Christian Fledelius ,  Birgitte Gissel ,  Birgit S Hansen ,  Niels Korsgaard ,  Susan M Thorpe ,  Karsten Wassermann
Affiliations
PMID: 11738615 DOI: 10.1016/s0968-0896(01)00257-7
Abstract

The syntheses and in vitro pharmacological evaluation of a number of cis-3,4-diaryl-hydroxy-chromanes are reported, along with the results of a thorough in vivo profiling of the tissue-selective estrogen partial-agonist NNC 45-0781 [3, (-)-(3S,4R)-7-hydroxy-3-phenyl-4-(4-(2-pyrrolidinoethoxy)phenyl)chromane]. These studies showed that NNC 45-0781 is a very promising candidate for the prevention of post-menopausal Osteoporosis, and the treatment of other health issues related to the loss of endogenous estrogen production.

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