2004
Estrogen to Antiestrogen with a Single Methylene Group Resulting in an Unusual Steroidal Selective Estrogen Receptor Modulator
Zhang JX, Labaree DC, Mor G, Hochberg RB. Estrogen to Antiestrogen with a Single Methylene Group Resulting in an Unusual Steroidal Selective Estrogen Receptor Modulator. The Journal Of Clinical Endocrinology & Metabolism 2004, 89: 3527-3535. PMID: 15240642, DOI: 10.1210/jc.2003-032005.Peer-Reviewed Original ResearchMeSH KeywordsAnimalsBody WeightBone and BonesCell Line, TumorCholesterolDose-Response Relationship, DrugEstradiolEstrogen AntagonistsEstrogen Receptor alphaEstrogen Receptor betaEstrogensFemaleHumansHydrocarbonsMethaneOrgan SizeRatsRats, Sprague-DawleyReceptors, EstrogenSelective Estrogen Receptor ModulatorsTransfectionUterusConceptsSelective estrogen receptor modulatorsEstrogen receptor modulatorsReceptor modulatorsBreast cancer preventionEstradiol-induced proliferationER affinityHigh ER affinityImportant therapeutic agentsPlasma cholesterolER alphaCancer preventionEstrogen agonistEstrogenic agonistTherapeutic agentsEstradiol analogsHigh estrogenic potencyCell bioassayBone growthEstrogenic activityAntiestrogensEstrogenic potencyAgonistsCritical structuresUnique mechanismGroup
2003
Synthesis and Evaluation of B-, C-, and D-Ring-Substituted Estradiol Carboxylic Acid Esters as Locally Active Estrogens
Labaree DC, Zhang JX, Harris HA, O'Connor C, Reynolds TY, Hochberg RB. Synthesis and Evaluation of B-, C-, and D-Ring-Substituted Estradiol Carboxylic Acid Esters as Locally Active Estrogens. Journal Of Medicinal Chemistry 2003, 46: 1886-1904. PMID: 12723952, DOI: 10.1021/jm0204340.Peer-Reviewed Original ResearchMeSH KeywordsAnimalsBinding, CompetitiveEsterasesEstersEstradiolEstradiol CongenersEstrogen Receptor alphaEstrogen Receptor betaFemaleHumansIn Vitro TechniquesKidneyLigandsMiceMicrosomesOrgan SizeOxidoreductasesRatsRats, Sprague-DawleyReceptors, EstrogenStructure-Activity RelationshipTumor Cells, CulturedUterusVaginaConceptsEstrogen receptorHormonal activityReceptor bindingAnalogues of estradiolEstrogen-sensitive genesEstrogen receptor bindingEstrogen-responsive genesEstrogenic actionIshikawa cellsEffective estrogenActive estrogensEstrogenHormonal actionDerivatives of estradiolEstradiolEstrogenic responsesSystemic actionReceptorsEstrogenic activityVivo assaysNonspecific esterasesSteroid nucleusSensitive genesActivitySteroid ring