Synthesis and estrogen receptor binding affinities of novel pyrrolo[2,1,5-cd]indolizine derivatives |
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| Authors: | Jørgensen A S Jacobsen P Christiansen L B Bury P S Kanstrup A Thorpe S M Naerum L Wassermann K |
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| Institution: | 1. School of Pharmacy, The University of Queensland, 20 Cornwall St, Woolloongabba, QLD 4102, Australia;2. School of Chemistry and Molecular Biosciences, The University of Queensland, St Lucia, QLD 4072, Australia;3. Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Helwan University, Ein Helwan, Helwan, Egypt;4. The University of Queensland Diamantina Institute, Translational Research Institute (TRI), Woolloongabba, QLD 4102, Australia;5. Griffith Health Institute and School of Medical Sciences, Griffith University, Southport, QLD 4222, Australia;6. Institute for Molecular Bioscience, The University of Queensland, St Lucia, QLD 4072, Australia;1. Department of Molecular Genetics, University of Lodz, Lodz 90-236, Poland;2. Department of Pharmaceutical Sciences, Nesbitt School of Pharmacy, Wilkes University, 84 W. South Street, Wilkes-Barre, USA;1. Center of Organic Chemistry ‘C.D. Nenitescu’ of Romanian Academy, 202B Splaiul Independentei, Sector 6, 060021 Bucharest, Romania;2. Department of Technology and Catalysis, University of Bucharest, Faculty of Chemistry, 4-12 Regina Elisabeta Blv., Sector 3, 030018 Bucharest, Romania;3. Spectropole, Universite Aix Marseille, Campus Scientifique de Saint Jérôme, Service 511, F-13397 Marseille, France;4. ‘Ilie Murgulescu’ Institute of Physical Chemistry of the Romanian Academy, 202 Splaiul Independentei, Sector 6, 060021 Bucharest, Romania;1. Department of Biochemistry & Molecular Biology, Drexel University College of Medicine, Rooms 10302-10306, 245 North 15th Street, Philadelphia, PA 19102, USA;2. Cresset, New Cambridge House, Bassingbourn Road, Litlington, Cambridgeshire SG8 0SS, UK;1. Sumitomo Dainippon Pharma Co., Ltd., 33-94 Enoki, Suita, Osaka 564-0053, Japan;2. Sumitomo Dainippon Pharma Co., Ltd., 3-1-98 Kasugade-naka, Konohana-ku, Osaka 554-0022, Japan |
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| Abstract: | A series of pyrrolo2,1,5-cd]indolizine derivatives has been synthesized and evaluated as ligands for the estrogen receptor. Properly substituted mono- and di-hydroxy derivatives showed binding in the low nanomolar range in accordance with their structural resemblance to estrogen. |
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