Structure–Activity Relationship of <i>para</i>-Carborane Selective Estrogen Receptor β Agonists
David Sedlák, Tyler A. Wilson, Werner Tjarks, Hanna S. Radomska, Hongyan Wang, Jayaprakash Narayana Kolla, Zbigniew J. Leśnikowski, Alena Špičáková, Tehane Ali, Keisuke Ishita, Liva Harinantenaina, Sandip Vibhute, Dasheng Wang, Pavel Anzenbacher, Chad Bennett, Petr Bartůněk, Christopher C. Coss
Abstract
-carborane ERβ selective agonists measure favorably against clinically developed ERβ agonists and support further evaluation of carborane-based selective estrogen receptor modulators.
Topics & Concepts
ChemistryEstrogen receptorAgonistEstrogen receptor betaCarboraneReceptorEstrogen receptor alphaNuclear receptorStructure–activity relationshipEstrogenPharmacologyLigand (biochemistry)Functional selectivityStereochemistryBiochemistryInternal medicineTranscription factorIn vitroEndocrinologyBiologyGeneMedicineCancerBreast cancerRadiopharmaceutical Chemistry and ApplicationsBoron Compounds in ChemistryBone health and treatments