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