Synthesis and pharmacological evaluation of novel cis-3,4-diaryl-hydroxychromanes as high affinity partial agonists for the estrogen receptor. |
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| Authors: | Paul S Bury Lise B Christiansen Poul Jacobsen Anker S J?rgensen Anders Kanstrup Lars Naerum Steven Bain Christian Fledelius Birgitte Gissel Birgit S Hansen Niels Korsgaard Susan M Thorpe Karsten Wassermann |
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| Affiliation: | 1. Laboratory of Immunocytochemistry, Program of Anatomy and Developmental Biology, School of Medicine, University of Chile, Chile;2. Departamento de Biología, Universidad de Tarapacá, Chile;1. Institute of Marine Resources, Faculty of Science, Technology & Environment, Private Bag, Laucala Campus, Suva, Fiji;2. Sustainability Research Centre, University of the Sunshine Coast, Maroochydore DC, QLD, 4558, Australia;1. Department of Clinical and Experimental Biomedical Science ‘Mario Serio’, University of Florence, Viale Morgagni 50, 50134 Florence, Italy;2. Department of Chemistry ‘Ugo Schiff’, University of Florence, Via della Lastruccia 13, 50019 Sesto Fiorentino, Florence, Italy;3. Interdepartmental Center for Preclinical Development of Molecular Imaging (CISPIM), University of Florence, Viale Morgagni 85, 50134 Florence, Italy;4. Department of Clinical and Experimental Biomedical Science ‘Mario Serio’, University of Florence, Largo Brambilla 3, 50134 Florence, Italy;5. Azienda Ospedaliera Universitaria Careggi (AOUC), Largo Brambilla 3, 50134 Florence, Italy |
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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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