Novel coordinatively saturated platinum(II)compounds bearing C-linked carbohydrates were synthesized and characterized.The complexes exhibit bipyramidal trigonal geometry with a bidentate nitrogen ligand and ethylene ...Novel coordinatively saturated platinum(II)compounds bearing C-linked carbohydrates were synthesized and characterized.The complexes exhibit bipyramidal trigonal geometry with a bidentate nitrogen ligand and ethylene in the equatorial plane.The axial positions are occupied by a halide ligand X and a D-galactose or D-glucose derivative,linked either via C1 or C6.The compounds were designed for evaluation of the biological activity because they combine the steady coordinative saturation,the beneficial action of the modular sugar moiety and the organometallic nature of the Pt-sugar linkage,which is expected to be stable in the biological media,until the target is reached.The newly synthesized molecules were stable in mixed DMSO/aqueous solvents,able to bind DNA in vitro and exhibited a selective cytotoxic activity on cancer cells through apoptosis activation.展开更多
基金the MIUR for the financial support(PRIN2015–Prot.20154X9ATP).
文摘Novel coordinatively saturated platinum(II)compounds bearing C-linked carbohydrates were synthesized and characterized.The complexes exhibit bipyramidal trigonal geometry with a bidentate nitrogen ligand and ethylene in the equatorial plane.The axial positions are occupied by a halide ligand X and a D-galactose or D-glucose derivative,linked either via C1 or C6.The compounds were designed for evaluation of the biological activity because they combine the steady coordinative saturation,the beneficial action of the modular sugar moiety and the organometallic nature of the Pt-sugar linkage,which is expected to be stable in the biological media,until the target is reached.The newly synthesized molecules were stable in mixed DMSO/aqueous solvents,able to bind DNA in vitro and exhibited a selective cytotoxic activity on cancer cells through apoptosis activation.
