2006
Microwave‐Enhanced Nucleophilic Fluorination in the Synthesis of Fluoropyridyl Derivatives of [3,2‐c]Pyrazolo‐corticosteroids, Potential Glucocorticoid Receptor‐Mediated Imaging Agents.
Kahn M, Konde E, Dossou F, Labaree D, Hochberg R, Hoyte R. Microwave‐Enhanced Nucleophilic Fluorination in the Synthesis of Fluoropyridyl Derivatives of [3,2‐c]Pyrazolo‐corticosteroids, Potential Glucocorticoid Receptor‐Mediated Imaging Agents. ChemInform 2006, 37: no-no. DOI: 10.1002/chin.200639207.Peer-Reviewed Original Research
1999
7α-Iodo and 7α-Fluoro Steroids as Androgen Receptor-Mediated Imaging Agents
Labaree D, Hoyte R, Nazareth L, Weigel N, Hochberg R. 7α-Iodo and 7α-Fluoro Steroids as Androgen Receptor-Mediated Imaging Agents. Journal Of Medicinal Chemistry 1999, 42: 2021-2034. PMID: 10354410, DOI: 10.1021/jm990064o.Peer-Reviewed Original ResearchConceptsAndrogen receptorAndrogen-responsive reporter geneHigh androgenic activityImaging agentReceptor-mediated uptakeDHT 4Rat prostatic cytosolReceptor binding propertiesHigh affinityMale ratsRat prostateAndrogenic activityResponsive reporter geneProstatic cytosolDiagnostic imaging agentsReceptorsHigh binding activitySteroidsIodinated compoundBiological activityDegrees CHigher bindingMetabolic oxidationDHTBiological potency
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