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1.
J Inorg Biochem ; 70(2): 145-54, 1998 May.
Article in English | MEDLINE | ID: mdl-9666573

ABSTRACT

Three Cu(II) co-ordination compounds with a novel ligand, 5-formyluracil thiosemicarbazone (H3ut), have been synthesised and characterised by single-crystal X-ray diffraction and subsequently tested in vitro on human leukemic cells. The crystal structures revealed, in all three cases, a square pyramidal co-ordination geometry of the copper atom with the ligand lying on the basal plane and behaving as an SNO terdentate ligand. These three compounds have been tested on human leukemic cell line K562 and CEM. In these experiments the complexes have demonstrated to inhibit cell growth and one of them to induce apoptosis. In the paper we also report the spectrophotometric characterization of the free ligand.


Subject(s)
Copper , Organometallic Compounds/chemical synthesis , Uracil/analogs & derivatives , Apoptosis/drug effects , Cell Division/drug effects , Cell Survival/drug effects , Crystallography, X-Ray , Humans , Leukemia , Models, Molecular , Organometallic Compounds/chemistry , Organometallic Compounds/toxicity , Thiosemicarbazones/chemical synthesis , Thiosemicarbazones/chemistry , Thiosemicarbazones/toxicity , Tumor Cells, Cultured , Uracil/chemical synthesis , Uracil/chemistry , Uracil/toxicity
2.
J Inorg Biochem ; 68(4): 295-305, 1997 Dec.
Article in English | MEDLINE | ID: mdl-9397578

ABSTRACT

A series of organotin complexes with pyrrole-2-carboxaldehyde 2-hydroxybenzoylhydrazone (H3mfps) and pyrrole-2-carboxaldehyde 2-picolinoylhydrazone (H2mfpp) was investigated. The IR, 1H, and 119Sn nuclear magnetic resonance spectroscopic characterization of all the compounds is reported and discussed in connection with the ligand behaviour of the hydrazone and the structure of the organotin complex. Complexes exhibit antibacterial properties higher than those of the corresponding ligands but they turn out to be less potent than the parent organotin compounds. Sn(H3mfps) (C6H5)2Cl2.2H2O and Sn(Hmfpp)(n-C4H9)2Cl are the most active antibacterial compounds showing MIC values between 3-6 micrograms/ml against Bacillus subtilis and Staphylococcus aureus and between 6-25 micrograms/ml against Escherichia coli; the first compound also strongly inhibits the growth of Aspergillus niger. All the ligands and complexes are devoid of DNA-damaging activity in the Bacillus subtilis rec-assay. H2mfpp and its complexes Sn(Hmfpp)(C2H5)2Cl and Sn3(Hmfpp)(mfpp) (C6H5)3Cl6 are shown by the Salmonella-microsome assay to be mutagenic substances in the presence of a metabolic activation system. The obtained results are discussed on the basis of structure-activity relationships.


Subject(s)
Bacteria/drug effects , Hydrazones/chemical synthesis , Mutagens , Organotin Compounds/chemical synthesis , Pyrroles/chemical synthesis , Aspergillus niger/drug effects , Bacillus subtilis/drug effects , Bacillus subtilis/genetics , Candida/drug effects , DNA Damage , Electrochemistry , Escherichia coli/drug effects , Fungicides, Industrial , Gram-Negative Bacteria/drug effects , Gram-Positive Bacteria/drug effects , Hydrazones/chemistry , Hydrazones/pharmacology , Magnetic Resonance Spectroscopy , Molecular Structure , Organotin Compounds/chemistry , Organotin Compounds/pharmacology , Pyrroles/chemistry , Pyrroles/pharmacology , Salmonella typhimurium/drug effects , Software , Staphylococcus aureus/drug effects , Structure-Activity Relationship
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