RESUMO
Plasma NO-binding activity was studied in patients with various forms of hematological malignancies. The method used in the study quantitatively evaluated the plasma capacity to bind NO, which reflects the intensity of NO production and the degree of patient's stress resistance. Plasma NO-binding activity significantly decreases in patients with hematological malignancies. Glucocorticoid treatment promotes the decrease in plasma NO-binding activity, which was dose-dependent.
Assuntos
Glucocorticoides/farmacologia , Neoplasias Hematológicas/sangue , Óxido Nítrico/sangue , Adolescente , Adulto , Idoso , Feminino , Glucocorticoides/uso terapêutico , Neoplasias Hematológicas/tratamento farmacológico , Humanos , Masculino , Pessoa de Meia-Idade , Ligação ProteicaRESUMO
Selected 7-alkylidene substituted cephems were synthesized and subjected to antitumor assay. The effect of substituents was examined to establish structure-activity relationships. It was found that the intensive intracellular generation of nitric oxide induced by tert-butyl 7-alkylidene cephalosporanate sulfones could be also regarded as an additional cytotoxic factor taking place both in vitro and in vivo experiments.
Assuntos
Antineoplásicos/síntese química , Antineoplásicos/farmacologia , Cefalosporinas/síntese química , Cefalosporinas/farmacologia , Animais , Antineoplásicos/química , Cefalosporinas/química , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Espectroscopia de Ressonância Magnética , Camundongos , Espectrofotometria Infravermelho , Relação Estrutura-Atividade , Células Tumorais CultivadasRESUMO
The [2+3] dipolar cycloaddition of nitrile oxides to the double C = C bonds of thiophene-1, 1-dioxides leads to formation of the fused isoxazolines-2 (1, 2). Tumor growth inhibition of these compounds strongly depends on the nature of group IV A element increasing from slightly active tert-butyl derivatives to silicon and germanium containing analogues. The products of benzonitrile oxide cycloaddition have greater cytotoxic effect than the compounds obtained from the cycloaddition reaction of 2, 5-disubstituted thiophene-1, 1-dioxides with acetonitrile oxide. Fused silyl substituted isoxazolines-2 are stronger NO-inducers than their germyl and tert-butyl analogues.
