RESUMO
3Beta,11beta-dihydroxy-9alpha-fluor-5alpha-androstane-17-one (2), 3beta-acetoxy-9alpha-fluor-11beta-hydroxy-5alpha-androstane-17-one (3), 3beta-acetoxy-9alpha-fluor-11beta,17beta-dihydroxy-5alpha-androstane (4), 3beta,17beta-diacetoxy-9alpha-fluor-11beta-hydroxy-5alpha-androstane (5), 3beta-acetoxy-9alpha-fluor-11beta-hydroxy-5alpha-androstane 17beta-propionate (6), 3beta-acetoxy-9alpha-fluor-11beta-hydroxy-5alpha-androstane 17beta-enanthate (7), 3beta-acetoxy-9alpha-fluor-11beta-hydroxy-5alpha-androstane 17beta-isobutyrate (8) were synthesized in the present study. Compounds 2 and 8 exhibited higher anabolic activity than the rest of the synthesized compounds. The structure of all these newly synthesized compounds was confirmed by analytic spectral data (mass, (1)H NMR and (13)C NMR).
Assuntos
Anabolizantes/química , Anabolizantes/farmacologia , Androgênios/química , Androgênios/farmacologia , Androstanos/química , Androstanos/farmacologia , Anabolizantes/síntese química , Androgênios/síntese química , Androstanos/síntese química , Animais , Flúor/química , Flúor/farmacologia , Masculino , Músculos/efeitos dos fármacos , Tamanho do Órgão/efeitos dos fármacos , Próstata/efeitos dos fármacos , Ratos , Ratos Wistar , Glândulas Seminais/efeitos dos fármacosRESUMO
We report the synthesis of the triphosphate of 5-methyl 4-N-[6-(p-bromobenzamido)hex-1-yl]-2'-O-deoxycytidine 3A. We also analyzed the formation of intramolecular H-bonds of 5-methyl 4-N-[n-[6-(p-bromobenzamido) caproyl amino]alk-1-yl]-2'-deoxycytidine compounds, and confirmed their presence by 1H-NMR studies. In vitro DNA labeling with modified nucleotides is preliminarily evaluated.
Assuntos
DNA/análise , DNA/metabolismo , Desoxicitidina/análogos & derivados , Desoxicitidina/síntese química , Desoxicitidina/metabolismo , Desoxicitidina/química , Escherichia coli , Ligação de Hidrogênio , Immunoblotting , Espectroscopia de Ressonância Magnética , Plasmídeos/metabolismo , Espectrometria de Massas de Bombardeamento Rápido de ÁtomosRESUMO
Nemorosone, the major constituent of the floral resin of Clusia rosea was isolated after exhaustive chromatography. This compound was fully characterized as it is in the nature, without methylation as reported before. A keto-enol equilibrium was observed and both isomers were totally characterized by NMR spectroscopic techniques. The previously announced structure for methylnemorosone was corrected on the basis of application of chemical methylation, high field 2D NMR techniques and NOE difference spectroscopy experiments on the natural product. Our studies concluded that an interchange occurred in the assignment of the benzoyl moiety position with an isoprenyl group in that structure.
Assuntos
Benzofenonas/isolamento & purificação , Rosales/química , Benzofenonas/química , Espectroscopia de Ressonância Magnética , Estrutura Molecular , Espectrometria de Massas por Ionização por ElectrosprayRESUMO
The introduction of 6-(p-bromobenzoylamino)caproyl radical in the methyl group of 2'-O-deoxythymidine is described. In vivo incorporation of this nucleoside to DNA was determined using a monoclonal antibody that recognized the radical.
