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Antineoplastic and cytogenetic effects of complexes of Pd (II) with 4N-substituted derivatives of 2-acetyl-pyridine-thiosemicarbazone.

The effect of novel Pd(II) complexes with derivatives of 2-acetyl-pyridinethisemicarbazone, N4-ethyl (HAc4Et) and 3-hexamethyleneiminylthiosemicarbazone (HAchexim), on Sister Chromatid Exchange (SCE) rates and human lymphocyte proliferation kinetics was studied. Also, the effect of Pd(II) complexes on DNA synthesis of P388 and L1210 cell cultures and against Leukemia P388 was investigated. Among these compounds, the compound Bis(3-hexamethyleneiminyl-2-acetylpyridine-thisemicarbazonato++ +) palladium (II) was found to be distinctly effective against Leukemia P388, in inhibiting incorporation of 3H-thymidine into DNA and in inducing SCEs and cell division delays.

Animals↗
PubMed2002

Evidence of desulfurization in the oxidative cyclization of thiosemicarbazones. Conversion to 1,3,4-oxadiazole derivatives.

The addition of pyridine-2-carbaldehyde 4N-methylthiosemicarbazone (C8H10N4S) to an aqueous solution of copper(II) nitrate yields [[Cu(C8H9N4S)(NO3)]2] (1). This complex consists of centrosymmetric dinuclear entities containing square-pyramidal copper(II) ions bridged through the sulfur thioamide atoms. The oxidation of 1 with KBrO3 or KIO3 gives rise to a compound with formula [[Cu(C8H8N4O)(H2O)2(SO4)]2]*2H2O (2) (C8H8N4O = 2-methylamino-5-pyridin-2-yl-1,3,4-oxadiazole). The structure of 2 is made up of centrosymmetric dimers where the copper(II) ions exhibit a distorted octahedral coordination and are connected by the oxadiazole moiety. The metal ions in 2 can be removed by addition of K4[Fe(CN)6], and then the oxadiazole ligand can be isolated and recrystallized as (C8H8N4O)*3H2O (3).

Journal Article↗
PubMed2004

Acetylacetonate bis(thiosemicarbazone) complexes of copper and nickel: towards new copper radiopharmaceuticals.

A series of copper(II) and nickel(II) 1,3-bis(thiosemicarbazonato) complexes have been synthesised by the reaction of the metal acetates with pyrazoline proligands. In each case the complexes have an overall neutral charge with a dianionic ligand. The copper 1,3-bis(4-methyl-3-thiosemicarbazonato complex has been characterised by X-ray crystallography, which shows the copper is in an essentially square-planar symmetric N(2)S(2) environment. The nickel 1,3-bis(4-methyl-3-thiosemicarbazonato) and nickel 1,3-bis(4-phenyl-3-thiosemicarbazonato) complexes have been characterised by X-ray crystallography and show that in these cases the nickel is in a distorted square-planar environment, but the bonding mode of the ligands is unusual; the nickel binds to one of the aza-methinic nitrogen atoms and one hydrazinic nitrogen, creating one five-membered N-N-C-S-Ni chelate ring and one four-membered N-C-S-Ni chelate ring. Interestingly, the X-ray structure of the ethyl analogue [1,3-bis(4-ethyl-3-thiosemicarbazonato)nickel(II)] shows that in this case the nickel is symmetrically coordinated in the usual manner. The nickel complexes are diamagnetic and the different coordination modes are confirmed in solution by NMR spectroscopy. The complexes are susceptible to oxidation in air and a nickel complex, in which the central methylene carbon has been oxidised, has been characterised by X-ray crystallography and NMR spectroscopy. Electrochemical measurements show that the copper complexes undergo a reversible one-electron reduction at biologically accessible potentials.

Journal Article↗
PubMed2002

Di-2-pyridyl ketone N4,N4-(butane-1,4-diyl)thiosemicarbazone.

The title compound, C(16)H(17)N(5)S, is in the thione form and crystallizes with two independent molecules in the asymmetric unit. In both molecules, the pentamethyleneimine five-membered ring adopts an envelope conformation, and in one of the molecules this ring shows positional disorder. The thione S and hydrazine N atoms are in the Z configuration with respect to the C-N bond.

Journal Article↗
PubMed1992

[Synthesis and bacteriostatic activity of new thiosemicarbazone derivatives--amino mercaptotriazole Schiff bases].

4-amino-3-(furan-2)-5-mercapto-1,2,4-triazole (Ia) and its ten Schiff bases derived from Ia with different aldehydes were synthesized. All the compounds were screened for activity against seven bacteria and three fungi. Most compounds were found to possess different inhibition effect on some bacteria and fungi. The azomethine group of Schiff bases is the active functional group and the substituted groups on the phenyl ring had definite effect on the bacteriostatic and fungistatic activities. 4-(5-Nitrofurfurylideneamino)-3-(furan-2)-5-mercapto-1,2,4-tria zol e (Ik) showed the most powerful antibacterial activity and broad antibacterial spectrum, while 4-salicylideneamino-3-(furan-2)-5-mercapto-1,2,4-triazole possessed strong activity against fungi.

Anti-Bacterial Agents↗