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
1998
Iodinated and fluorinated steroid 2′-aryl-[3,2-c] pyrazoles as potential glucocorticoid receptor imaging agents
Hoyte R, Labaree D, Fede J, Harris C, Hochberg R. Iodinated and fluorinated steroid 2′-aryl-[3,2-c] pyrazoles as potential glucocorticoid receptor imaging agents. Steroids 1998, 63: 595-602. PMID: 9830686, DOI: 10.1016/s0039-128x(98)00069-5.Peer-Reviewed Original ResearchConceptsPotent glucocorticoidGlucocorticoid receptorTrihydroxy-16Potential glucocorticoid receptorReceptor imaging agentImaging agentPositron emission tomographyHeLa cell assayGlucocorticoid potencyEmission tomographySteroidsGlucocorticoidsReceptorsCell assayDexamethasoneAlkaline phosphataseSteroids 2PotencyAgentsPara positionBromo analogueBest ligandSide chainsCortivazolFluoro analogue