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

…, C Fledelius, B Gissel, BS Hansen, N Korsgaard…

Index: Bury, Paul S.; Christiansen, Lise B.; Jacobsen, Poul; Jorgensen, Anker S.; Kanstrup, Anders; Narum, Lars; Bain, Steven; Fledelius, Christian; Gissel, Birgitte; Hansen, Birgit S.; Korsgaard, Niels; Thorpe, Susan M.; Wassermann, Karsten Bioorganic and Medicinal Chemistry, 2002 , vol. 10, # 1 p. 125 - 145

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Citation Number: 28

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 ...