6533b85efe1ef96bd12bf514
RESEARCH PRODUCT
17 beta-carboxamide steroids: highly effective inhibitors of the phytohaemagglutinin mediated blastogenesis of normal human peripheral lymphocytes.
Marianne RehderR. KreienbergKunhard PollowA. HeubnerBernhard ManzHans-jörg Grillsubject
Malemedicine.medical_specialtyChemical Phenomenamedicine.drug_classClinical BiochemistryeducationCarboxamideBiologyIn Vitro TechniquesLymphocyte ActivationBinding CompetitiveDexamethasoneGlucocorticoid receptorCytosolReceptors GlucocorticoidInternal medicinemedicinePotencyAnimalsHumansPhytohemagglutininsBeta (finance)GlucocorticoidsDexamethasonePhytohaemagglutininBiochemistry (medical)Biological activityRats Inbred StrainsGeneral MedicineDNAPeripheralRatsChemistryEndocrinologyLiverbiology.proteinmedicine.drugThymidinedescription
Several novel 17 beta-carboxamide analogues of dexamethasone were synthesized. The common precursor, 9-fluoro-16 alpha-methyl-11 beta,17-dihydroxy-3-oxo-1,4-androstadiene-17 beta-carboxylic acid, did not bind to the glucocorticoid receptors of rat liver and human spleen tumours. In addition, no inhibition of the mitogen-induced blastogenesis of cultured human peripheral lymphocytes was observed. The 17 beta-carboxamide analogues, however, bound with similar affinities to the glucocorticoid receptors of both tissues. They inhibited the mitogen-induced blastogenesis of peripheral lymphocytes, showing the same potency and same order of binding affinity as the natural glucocorticoids.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 1984-03-01 | Journal of clinical chemistry and clinical biochemistry. Zeitschrift fur klinische Chemie und klinische Biochemie |