2012
Targeting the estrogen receptor with metal-carbonyl derivatives of estradiol
Hanson RN, Kirss R, McCaskill E, Hua E, Tongcharoensirikul P, Olmsted SL, Labaree D, Hochberg RB. Targeting the estrogen receptor with metal-carbonyl derivatives of estradiol. Bioorganic & Medicinal Chemistry Letters 2012, 22: 1670-1673. PMID: 22277281, PMCID: PMC3274643, DOI: 10.1016/j.bmcl.2011.12.111.Peer-Reviewed Original Research
2001
Estradiol-16α-carboxylic Acid Esters as Locally Active Estrogens
Labaree D, Reynolds T, Hochberg R. Estradiol-16α-carboxylic Acid Esters as Locally Active Estrogens. Journal Of Medicinal Chemistry 2001, 44: 1802-1814. PMID: 11356114, DOI: 10.1021/jm000523h.Peer-Reviewed Original ResearchMeSH KeywordsAlkaline PhosphataseAnimalsBinding, CompetitiveEnzyme InductionEstersEstradiolEstradiol CongenersEstrogen Receptor alphaEstrogen Receptor betaFemaleHumansIn Vitro TechniquesMiceMicrosomes, LiverOrgan SizeOvariectomyOxidoreductasesRatsRats, Sprague-DawleyReceptors, EstrogenStructure-Activity RelationshipTumor Cells, CulturedUterusVaginaConceptsEstrogenic actionActive estrogensAnalogues of estradiolRat uterine weightEstrogenic potencyEstrogen receptor bindingSystemic estrogenRat hepatic microsomesUterine weightIshikawa cellsVivo modelEstrogenTherapeutic treatmentHepatic microsomesReceptor bindingFluoroethyl esterSystemic actionER affinityHigh ER affinityEstradiolEsterase hydrolysisPotencyDyspareuniaLocal actionMenopause