Pyrazolo[1,5-a]pyrimidines as estrogen receptor ligands: defining the orientation of a novel heterocyclic core |
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Authors: | Compton Dennis R Carlson Kathryn E Katzenellenbogen John A |
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Affiliation: | Department of Chemistry, University of Illinois, 600 S. Matthews Avenue, Urbana, IL 61801-3731, USA. |
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Abstract: | We have examined the pyrazolo[1,5-a]pyrimidine scaffold as a novel core structure for estrogen receptor ligands. Attachment of various substituents has helped to define the orientation of this heterocycle in the ligand-binding pocket as one in which a pendant phenol rather than the hydroxylpyrimidine serves as a mimic of the A-ring of estradiol. |
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