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
1990
A Simple and Sensitive Microtiter Plate Estrogen Bioassay Based on Stimulation of Alkaline Phosphatase in Ishikawa Cells: Estrogenic Action of Δ5 Adrenal Steroids*
Littlefield BA, Gurpide E, Markiewicz L, McKinley B, Hochberg RB. A Simple and Sensitive Microtiter Plate Estrogen Bioassay Based on Stimulation of Alkaline Phosphatase in Ishikawa Cells: Estrogenic Action of Δ5 Adrenal Steroids*. Endocrinology 1990, 127: 2757-2762. PMID: 2249627, DOI: 10.1210/endo-127-6-2757.Peer-Reviewed Original ResearchConceptsEstrogenic actionIshikawa cellsHuman endometrial adenocarcinoma cell lineEndometrial adenocarcinoma cell lineAction of estradiolDelta 5Ishikawa human endometrial adenocarcinoma cell lineType of steroidAdenocarcinoma cell lineAdrenal steroidsEstrogen bioassayAdrenal delta 5Aromatase inhibitorsEstrogenC19 steroidsAlkPEstradiolSteroidsDelta 4StimulationAntiestrogensCell linesDehydrogenase inhibitorAlkaline phosphataseAlkaline phosphatase enzyme activity