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

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
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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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