RESUMO
Bismuth dithiocarbamate complexes of general formula Bi(S(2)CNR(2))(3) demonstrate potent in vitro cytotoxicity against a panel of seven human cancer cell lines; a structure-activity relationship has been established. Potency exhibited by the R=Et (2) derivative, for example, is unrivalled by standard cancer drugs with the exception of paclitaxel. In vivo studies indicate a significant anti-tumor effect exerted by (2) against both OVCAR-3, an ovarian cancer cell line, and HT-29, a colon carcinoma cell line.
Assuntos
Bismuto/farmacologia , Compostos Organometálicos/química , Compostos Organometálicos/farmacologia , Tiocarbamatos/química , Tiocarbamatos/farmacologia , Animais , Bismuto/química , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Neoplasias do Colo/tratamento farmacológico , Feminino , Células HT29 , Humanos , Espectroscopia de Ressonância Magnética , Masculino , Camundongos , Camundongos Endogâmicos BALB C , Camundongos Nus , Compostos Organometálicos/síntese química , Neoplasias Ovarianas/tratamento farmacológico , Relação Quantitativa Estrutura-Atividade , Distribuição Aleatória , Espectrofotometria Infravermelho , Tiocarbamatos/síntese química , Ensaios Antitumorais Modelo de XenoenxertoRESUMO
The partial conversion of methanol (MeOH) to formaldehyde (HCHO) in the gas chromatograph (GC) injection port was studied. The presence of formaldehyde in the injection port can result in reaction with injected analytes, especially primary and secondary amines. A systematic study of this problem was undertaken using norephedrine and ephedrine as probe analytes, and experiments involving varying inlet temperature, comparisons among solvents and solvent mixtures, isotopic labeling, and formaldehyde spiking. These experiments showed a direct correlation between inlet temperature and formation of the amine-formaldehyde condensation products. The mass spectra of the norephedrine and ephedrine condensation products were consistent with addition of the methylene group derived from formaldehyde across the amine and alcohol moieties to form the corresponding oxazolidine-ring compounds. Results for the imine condensation product of didesmethylsibutramine formed in the injection port are also presented.