Platinum(II) and Palladium(II) Complexes of Pyridine-2-Carbaldehyde Thiosemicarbazone as Alternative Antiherpes Simplex Virus Agents

The cytotoxicity and the antivirus activity of Pd(II) and Pt(II) complexes with pyridine-2-carbaldehyde thiosemicarbazone (HFoTsc) against HSV replication were evaluated on four HSV strains—two wt strains Victoria (HSV-1) and BJA (HSV-2) and two ACVR mutants with different tk gene mutations R-100 (TKA, HSV-1) and PU (TKN, HSV-2). The experiments were performed on continuous MDBK cells and four HSV 1 and HSV 2 strains were used, two sensitive to acyclovir and two resistant mutants. The five complexes of HFoTsc, [Pt(FoTsc)Cl], [Pt(FoTsc)(H2FoTsc)]Cl2, [Pt(FoTsc)2], [Pd(FoTsc)(H2FoTsc)]Cl2, and [Pd(FoTsc)2], were found to be effective inhibitors of HSV replication. The most promising, active, and selective anti-HSV agent was found to be complex [Pt(FoTsc)(H2FoTsc)]Cl2. This complex could be useful in the treatment of HSV infections, since it is resistant to ACV mutants. PCR study of immediate early 300 bp ReIV Us1 region reveals that the complex [Pt(FoTsc)(H2FoTsc)]Cl2 specifically suppressed wt HSV-1 genome 2 hours after the infection, not inducing apoptosis/necrosis on the 8 hours after virus infection. The target was found to be most probably the viral, instead of the host cell DNA

Cytotoxic activities of new iron(III) and nickel(II) chelates of some S-methyl-thiosemicarbazones on K562 and ECV304 cells

The S-methyl-thiosemicarbazones of the 2- hydroxy-R-benzaldehyde (R= H, 3-OH 3-OCH3 or 4-OCH3) reacted with the corresponding aldehydes in the presence of FeCl3 and NiCl2. New ONNO chelates of iron(III) and nickel (II) with hydroxy- or methoxy-substitued N1,N4-diarylidene-Smethyl- thiosemicarbazones were characterized by means of elemental analysis, conductivity and magnetic measurements, UV-Vis, IR and 1H-NMR spectroscopies. Cytotoxic activities of the compounds were determined using K562 chronic myeloid leukemia and ECV304 human endothelial cell lines by MTT assay. It was determined that monochloro N1-4- methoxysalicylidene-N4-4-methoxysalicylidene-S-methylthiosemicarbazidato- iron(III) complex showed selective anti-leukemic effects in K562 cells while has no effect in ECV304 cells in the 0.53 μg/ml (IC50) concentrations. Also, some methoxy-substitued nickel(II) chelates exhibit high cytotoxic activitiy against both of these cell lines in low concentrations. Cytotoxicity data were evaluated depending on cell lines origin and position of the substituents on aromatic rings

In vitro antitumor activity of 2-acetyl pyridine 4n-ethyl thiosemicarbazone and its platinum(II) and palladium(II) complexes

The reaction of platinum(II) [Pt(II)] or palladium(II) [Pd(II)] with 2-acetyl pyridine 4N-ethyl thiosemicarbazone, HAc4Et (1) results in the complexes [Pt(Ac4Et) 2 ] (2) and [Pd(Ac4Et) 2 ] (3). In a panel of human tumor cell lines of different origins (breast, colon, and ovary cancers), and containing also cisplatin-refractory/resistant cell lines, the in vitro growth inhibitory effect of 1–3 was compared to that of cisplatin by using the sulforodamine B assay. After a 96-hour continuous treatment, both the thiosemicarbazone HAc4Et and the metal compounds [Pt(Ac4Et) 2 ] and [Pd(Ac4Et) 2 ] exhibit very remarkable growth inhibitory activities with mean IC 50 values of 0.9 n M (0.22– 2.47 n M ), 0.7 n M (0.15–2 n M ) and 0.5 n M (0.17–1.02 n M ), respectively. In contrast, cisplatin shows a markedly lower growth inhibitory potency, the mean IC 50 in the panel being 2.8 _ M (0.2–8 _ M ). In addition to their major cell growth inhibitory potency, complexes 1–3 are characterized by a growth inhibitory profi le different from that of cisplatin, being active towards cisplatin-refractory tumor cell lines. These fi ndings, along with the ability of completely overcoming acquired cisplatin resistance from either multifocal or reduced uptake origin, confi rm the antitumor potential of HAc4Et and support the hypothesis that both [Pt(Ac4Et) 2 ] and [Pd(Ac4Et) 2 ] complexes can be characterized by cellular pharmacological properties distinctly different from those of cisplati

Adducts of organotin(IV), tin(IV) and tin(II) halides with 1-methyl-imidazoline-2(3H)-thione (Hmimt) and imidazoline-2(1,3H)-thione (Himt). Synthesis, spectroscopic (IR, Mössbauer and H-1, C-13, Sn-119 NMR) studies and in vitro antitumour activity

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Variation of product identity as a function of metal ion: ligand reaction ratio, stereochemical studies and thermal investigation of Mn(II), Fe(III), N

A systematic investigation of the MX2 and FeCl3/APH reaction systems in EtOH is described, where M = Mn, Ni, Cu, Cd and Hg, X = Cl, Br, NO3, SCN, CH3COO, BF4 and 1 2SO4, and APH = 2-acetylpyridine hydrazone. Emphasis has been placed on determining the influence of the metal ion : APH ratio on the identity of the reaction products. The variation of this ratio has led to the synthesis of thirty-two new discrete complexes with general compositions M(APH)X2, M(APH)2X2, M(APH)3X2, Fe(APH)Cl3 and Fe(APH)2Cl3. The complexes were characterized by elemental analyses, conductivity measurements. X-ray powder patterns, thermal methods, magnetic susceptibilities and spectroscopie (IR, ligand field, 1H NMR, ESR) studies. Monomeric pseudo-tetrahedral and monomeric or polymeric distorted octahedral stereochemistries were assigned in the solid state. APH appears to coordinate via both the pyridine and methine nitrogen atoms. The thermal decomposition of the prepared complexes was also studied. Some Ni(II) complexes decompose via stable intermediates. Probable mechanistic paths of the decomposition reactions have been proposed. © 1989