RESUMEN
[1,1-Cyclobutanedicarboxylato(2)-O,O'](1,3-dioxane-5,5-dimethan amine- N,N')platinum(II), 3a, a third generation, very water-soluble platinum complex, has been synthesized along with several of its analogues. All members of the new family contain a 1,3-dioxane or 1,3-dioxolane-1,3-diamine as their basic ligand, a moiety which contributes to their increased water solubility, and a bidentate acid ligand, which is responsible for their good stability. They were all easily crystallized and characterized by 1H NMR and elemental analysis, and the parent complex 3a was further characterized by 13C NMR. Their very desirable physical properties combined with their broad spectrum of antitumor activity and reduced toxicity make them good candidates of further development.
Asunto(s)
Antineoplásicos/síntesis química , Dioxanos/síntesis química , Dioxinas/síntesis química , Dioxolanos/síntesis química , Dioxoles/síntesis química , Compuestos Organoplatinos/síntesis química , Animales , Antineoplásicos/uso terapéutico , Carboplatino , Fenómenos Químicos , Química , Cisplatino/uso terapéutico , Dioxanos/uso terapéutico , Dioxolanos/uso terapéutico , Femenino , Humanos , Leucemia L1210/tratamiento farmacológico , Leucemia P388/tratamiento farmacológico , Neoplasias Mamarias Experimentales/tratamiento farmacológico , Melanoma Experimental/tratamiento farmacológico , Ratones , Ratones Endogámicos BALB C , Ratones Endogámicos C57BL , Compuestos Organoplatinos/uso terapéutico , Neoplasias Ováricas/tratamiento farmacológico , Solubilidad , Relación Estructura-ActividadRESUMEN
The synthesis, stability, and antitumor activity of a series of water-soluble third generation platinum(II) complexes have been described. Among these complexes, [2,2-bis(aminomethyl)-1,3- propanediol-N,N'] [1,1-cyclobutanedicarboxylato(2-)-O,O']platinum(II) and [1,1-cyclobutanedicarboxylate(2-)-O,O'](tetrahydro-4H-pyran-4,4- dimethanamine-N,N'-)platinum(II) have shown the greatest promise for further investigation and are currently under clinical evaluation.
Asunto(s)
Antineoplásicos/síntesis química , Carboplatino/análogos & derivados , Compuestos Organoplatinos/síntesis química , Animales , Antineoplásicos/uso terapéutico , Fenómenos Químicos , Química , Femenino , Humanos , Ratones , Ratones Desnudos , Modelos Moleculares , Trasplante de Neoplasias , Neoplasias Experimentales/tratamiento farmacológico , Compuestos Organoplatinos/uso terapéutico , Relación Estructura-ActividadRESUMEN
We report on the synthesis of N-1-phenylquinolones in which the difluoromethoxy moiety is utilized as a halogen replacement. The antibacterial activity is discussed with reference to N-1-halophenylquinolones.