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Eight novel Pt(II), Pd(II), Cu(II) and Zn(II) complexes with 4'-substituted terpyridine were synthesized and characterized by elemental analysis, UV, IR, NMR, electron paramagnetic resonance, high-resolution mass spectrometry and molar conductivity measurements. The cytotoxicity of these complexes against HL-60, BGC-823, KB and Bel-7402 cell lines was evaluated by MTT assay. All the complexes displayed cytotoxicity with low IC50 values (<20 μ m) and showed selectivity. Complexes 3, 5, 7 and 8 exerted 9-, 5-, 12- and 7-fold higher cytotoxicity than cisplatin against Bel-7402 cell line. The cytotoxicity of complexes 3, 5, 6, 7 and 8 was higher than that of cisplatin against BGC-823 cell line. Complexes 3, 7 and 8 showed similar cytotoxicity to cisplatin against KB cell line. Complex 7 exhibited higher cytotoxicity than cisplatin against HL-60 cell line. Among these complexes, complex 7 demonstrated the highest in vitro cytotoxicity, with IC50 values of 1.62, 3.59, 2.28 and 0.63 μ m against HL-60, BGC-823, Bel-7402 and KB cells lines, respectively. The results suggest that the cytotoxicity of these complexes is related to the nature of the terminal group of the ligand, the metal center and the leaving groups. Copyright © 2013 John Wiley & Sons, Ltd. [ABSTRACT FROM AUTHOR]

Eight new platinum(II)/palladium(II) complexes with 4-toluenesulfonyl-L-amino acid dianion and diimine/diamine ligands, [Pd(en)(Tsile)]·H2O (1), [Pd(bipy)(Tsile)] (2), [Pd(bipy)(Tsthr)]·0.5H2O (3), [Pd(phen)(Tsile)]·0.5H2O (4), [Pd(phen)(Tsthr)]·H2O (5), [Pd(bqu)(Tsthr)]·1.5H2O (6), [Pt(en)(Tsser)] (7), and [Pt(en)(Tsphe)]·H2O (8), have been synthesized and characterized by elemental analyses,1H NMR and mass spectrometry. The crystal structure of 7 has been determined by X-ray diffraction. Cytotoxicities were tested by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide and sulforhodamine B assays. The complexes exert cytotoxicity against HL-60, Bel-7402, BGC-823, and KB cell lines with 4 having the best cytotoxicity against HL-60, Bel-7402, and BGC-823 cell lines; the compounds are less cytotoxic than cisplatin. [ABSTRACT FROM AUTHOR]

Abstract: Eight novel platinum(II)/palladium(II) complexes with 1,3-dap and 4-toluensulfonyl-l-amino acid dianion, [Pt(1,3-dap)(TsalaNO)]·0.5H2O (1a), [Pt(1,3-dap)(TsvalNO)] (1b), [Pt(1,3-dap)(TspheNO)] (1c), [Pt(1,3-dap)(TsserNO)] (1d), [Pd(1,3-dap)(TsalaNO)]·1.5H2O (2a), [Pd(1,3-dap)(TsvalNO)] (2b), [Pd(1,3-dap)(TspheNO)] (2c) and [Pd(1,3-dap)(TsileNO)] (2d) have been synthesized and characterized by elemental analysis, IR, UV, 1H NMR and mass spectrometry techniques. Crystal structure of the complex 1b has been determined by X-ray diffraction. The cytotoxicity was tested by MTT and SRB assays. The complexes (1a–1d and 2a–2d) exert cytotoxicity against Bel-7402, HL-60, KB and BGC-823, but none of them is more active than cisplatin. The results suggest that metal ions, amino acids and aliphatic N-containing ligands have effect on cytotoxicity, while the IC50 values do not show definite correlation with variation of them. [Copyright &y& Elsevier]

Four new platinum(II) complexes (1–4) with N-benzoyl-L-amino acid and bipy were synthesized and characterized by elemental analysis, IR, UV, 1H NMR, and mass spectra. The crystal structure of 1 was determined by X-ray diffraction analysis. Cytotoxicities were measured by MTT and SRB assays. Complexes 1–4 exert cytotoxicity with selectivity against HL-60, Bel-7402, BGC-823, and KB cell lines. This suggests that amino acids and acylated groups have important effects on cytotoxicity; the cytotoxicity is also related to the species of tumor cells, but the IC50 values do not show definite correlation with the variation of amino acids and acylated groups. [ABSTRACT FROM PUBLISHER]

Five new palladium(II) complexes with 4-toluenesulfonyl-L-amino acid dianion and en, [Pd(en)(TsserNO)] (1), [Pd(en)(TsglyNO)] (2), [Pd(en)(TsalaNO)] · 1.5H2O (3), [Pd(en)(TsleuNO)] · H2O (4), and [Pd(en)(TspheNO)] · 2H2O (5), have been synthesized and characterized by elemental analysis, IR, UV, 1H NMR, and mass spectrometry. Crystal structure of 1 has been determined by X-ray diffraction analysis. The cytotoxicity was tested by MTT and SRB assays. The results indicate 1–5 exert cytotoxic effects against HL-60, Bel-7402, BGC-823, and KB cell lines and 5 displays the best cytotoxicity. The structure–activity relationships suggest that both amino acid and N-containing ligands have important effects on cytotoxicity. [ABSTRACT FROM PUBLISHER]

Abstract: Seven new palladium(II) complexes (1–7) with 4-toluenesulfonyl-L-amino acid dianion and 2, 2′-biquinoline (bqu)/1,4-diaminobutane (dab) have been synthesized and characterized by elemental analysis, IR, 1H NMR, and mass spectra techniques. Crystal structure of the complex (7) has been determined by X-ray diffraction analysis. The cytotoxicity was tested by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) and sulforhodamine B (SRB) assays. The results indicate that the complexes exert cytotoxic effects with selectivity against tested carcinoma cell lines, but their cytotoxicity is less than that of cisplatin. It suggests that all the amino acids, N-containing ligands and metal ions have important effect on cytotoxicity, but the IC50 values do not show definite correlation with variation of amino acids, N-containing ligands and metal ions, the cytotoxicity of complexes is related to tumor cell species. [Copyright &y& Elsevier]

Abstract: Eight new palladium(II) complexes (1a–2d) with 4-toluenesulfonyl-l-amino acid dianion and diimine (bipy and phen) have been synthesized and characterized by elemental analysis, IR, UV, 1H NMR, 13C NMR and mass spectra techniques. Crystal structure of the complex (2d) has been determined by X-ray diffraction analysis. The cytotoxicity was tested by MTT and SRB assays. The results indicate that the complexes (1a–2d) have selectivity against tested carcinoma cell lines. The complex (2c) has the best cytotoxicity among the eight complexes, moreover its cytotoxicity is better than that of cisplatin against BGC-823, Bel-7402 and KB cell lines. It suggests that both aromatic diimine and 4-toluenesulfonyl-l-amino acid have important effect on cytotoxicity. [ABSTRACT FROM AUTHOR]

Abstract: Seven new iodo-bridged binuclear platinum(II) complexes [Pt(L)I2]2 (1–7) (L = n-butylamine, isopropylamine, m-toluidine, p-toluidine, diethylamine, N-methylaniline and aniline) have been synthesized and characterized by elemental analysis, conductivity, thermal analysis, IR, 1H NMR and mass spectra techniques. The cytotoxicity was tested by MTT assay. The results indicate that they have selectivity against tested carcinoma cell lines. For example, the complexes (3 and 7) have better cytotoxicity than cisplatin against Bel-7402 cell line, the complexes (2–5 and 7) have better cytotoxicity than cisplatin against Hela cell line. The results suggest that the species of amine has important effect on cytotoxicity, when L = m-toluidine, p-toluidine and aniline, the complexes have better cytotoxicity against tested carcinoma cell lines. [Copyright &y& Elsevier]

Abstract: Six new type binuclear platinum(II) complexes (a–f) have been synthesized and characterized by elemental analysis, conductivity, thermal analysis, IR, UV, 1H NMR and mass spectra techniques. The cytotoxicity of the complexes was tested by MTT and SRB assays. The cell cycle analysis and the levels of total platinum bound to DNA were measured by flow cytometry and ICP-MS, respectively. The results indicate that the complex (a) has no cytotoxicity against HL-60, BGC-823, Bel-7402, KB and Hela, the complexes (b, c, e and f) have weaker cytotoxicity against some tested carcinoma cell lines, the complex (d) has better cytotoxicity against HL-60, BGC-823, Bel-7402, KB, MCF-7, HCT-8 and Hela with respect to the IC50 values obtained. The cytotoxicity of the complex (d) is equal to that of cisplatin against HL-60 and Bel-7402 (P >0.05), but it has better cytotoxicity than that of cisplatin against BGC-823 and MCF-7 (P <0.05). The complex (d) causes significant G2/M arrest and a concomitant decrease of cell population in G1 and S phases, and the total DNA platination levels of the complex (d) are higher than those of cisplatin under the same experimental conditions. It suggests that the bridging linker has important effect on their cytotoxicity. Indeed, when the bridging linker is dicarboxylic acid, their cytotoxicity is better than that of platinum complexes with an amino acid as bridging linker. The new type binuclear platinum(II) complexes represent a novel class of anticancer agents, which deserves further attention in search of anticancer lead compounds. [Copyright &y& Elsevier]

Four new ammine/cyclohexylamine platinum(II) complexes with dicarboxylates (a–d) have been synthesized and characterized by elemental analysis, conductivity, IR, UV, and 1 HNMR spectra techniques. The cytotoxicity of the complexes was tested by MTT assay. The cell cycle analysis and the levels of total platinum bound to DNA were measured by flow cytometry and ICP‐MS. The results show that the cytotoxicity of complexes (a–d) against EJ, HCT‐8, BGC‐823, HL‐60, and MCF‐7 cell lines decreases in the sequence: b>a>c>d. Complexes (a–d) have better cytotoxicity against EJ and HL‐60 and complex (b) demonstrates cytotoxicity superior to that of the clinically established cisplatin. The complexes (a–d) induced a concentration‐dependent accumulation of HL‐60 cells in the G 2 /M phase of the cell cycle as cisplatin. The levels of total platinum bound to DNA in HL‐60 and EJ cells decrease in the sequence: b>cisplatin>a>c>d under the same experimental conditions. [ABSTRACT FROM AUTHOR]

Lanthanide-doped sodium yttrium fluoride (NaYF 4 ) nanoparticles exhibit novel optical properties which make them be widely used in various fields. The extensive applications increase the chance of human exposure to these nanoparticles and thus raise deep concerns regarding their riskiness. In the present study, we have synthesized europium doped NaYF 4 (NaYF 4 :Eu 3 + ) nanoparticles with three diameters and used endothelial cells (ECs) as a cell model to explore the potential toxic effect. The cell viability, cytomembrane integrity, cellular uptake, intracellular localization, intracellular reactive oxygen species (ROS), mitochondrial membrane potential (MMP), apoptosis detection, caspase-3 activity and expression of inflammatory gene were studied. The results indicated that these nanoparticles could be uptaken into ECs and decrease the cell viability, induce the intracellular lactate dehydrogenase (LDH) release, increase the ROS level, and decrease the cell MMP in a size-dependent manner. Besides that, the cells were suffered to apoptosis with the caspase-3 activation, and the inflammation specific gene expressions (ICAM1 and VCAM1) were also increased. Our results suggest that the damage pathway may be related to the ROS generation and mitochondrial damage. The results provide novel evidence to elucidate their toxicity mechanisms and may be helpful for more rational applications of these compounds in the future. [ABSTRACT FROM AUTHOR]

Abstract: Pd(II), Cu(II) and Zn(II) complexes (1–3) based on 4′-(4-(2-(piperidin-1-yl)ethoxy)phenyl)-2,2′:6′,2″-terpyridine were synthesized and characterized by UV, IR, NMR, EPR, HRMS, elemental analyses, and molar conductivity measurements. The cytotoxicity of these complexes against HL-60, BGC-823, KB, Bel-7402, A549, Hela, K562 and MCF-7 cell lines in vitro was measured by MTT method. The DNA binding property of the complexes was evaluated by UV, fluorescence, CD spectroscopies and thermal denaturation. The cytotoxicity of complexes 1 and 3 against all the tested cell lines is better than that of cisplatin. Complexes 1 and 2 exhibit 7- and 4-folds higher cytotoxicity than cisplatin against Bel-7402 cell line. Complex 3 displays the highest cytotoxicity against all the cell lines tested, and shows 7-, 14-, 8-, 11- and 8-folds higher cytotoxicity than cisplatin against Bel-7402, A549, Hela, K562 and MCF-7 cell lines. The complexes bind to DNA via intercalation mode and complex 3 stabilizes the G-quadruplex. The results reveal that all the complexes display high cytotoxicity against all the tested cancer cell lines, and complex 3 is selective for G-quadruplex over duplex DNA. [Copyright &y& Elsevier]

Abstract: To investigate how the novel synthetic immunostimulators (CH1a, CH2a, CH1b and CH2b) with a core substructure of thiazolidin-4-one ring influence the function of human natural killer (NK) cells in vitro, first, we obtained highly purified and viable NK cells from peripheral blood mononuclear cells (PBMCs) by a magnetic cell sorter (MACS). Then, the cytotoxicity and proliferative capacity of NK cells were explored after treatment with CH1a, CH2a, CH1b and CH2b. Moreover, the production of IFN-γ and TNF-α was also analyzed. We found that CH1b and CH2b could induce a significant enhancement of cytotoxicity and cytokine production including IFN-γ and TNF-α by NK cells. However, CH1b and CH2b could hardly promote the proliferation of NK cells. In immunoblotting analysis assay, we found that ERK 1/2 could be significantly phosphorylated after treatment with CH1b and CH2b, while the same phenomenon did not emerge after blockade with PD098059, the specific inhibitor of ERK1/2 signaling pathways. Taken together, we can conclude that CH1b and CH2b can elevate the cytotoxicity probably via ERK 1/2 activation. [Copyright &y& Elsevier]

Abstract: Eight new gold(III) complexes (1–8) of 5-aryl-3-(pyridin-2-yl)-4,5-dihydropyrazole-1-carbothioamide have been synthesized and characterized by elemental analysis, molar conductivity, IR, UV, 1H NMR, 13C NMR, MS, and thermal analysis techniques. The cytotoxicity was tested by MTT assay. The results indicate that the complexes 1–8 exert cytotoxic effects against HeLa and A549 cell lines. Moreover, the complexes 1, 4, 5, 7 and 8 have higher cytotoxicity than cisplatin against HeLa cell line. It suggests that the substituent groups on benzene have important effect on cytotoxicity. [Copyright &y& Elsevier]

Abstract: A series of novel glycosyl thiazol-2-imines (3a–g) have been synthesized regioselectively in good yields from the hydrolysis of thiazol-2(3H)-imine-linked glycoconjugates. The glycosyl thiazol-2-imines were evaluated for their antitumor activity against Hela (cervical carcinoma), HCT-8 (colon carcinoma) and Bel-7402 (liver carcinoma). Among the compounds screened, 1-benzoyl-4-(4-nitrophenyl)-3-β-d-glucopyranosyl-thiazol-2(3H)-imine (3c) was found to be the most active compound against HCT-8. [Copyright &y& Elsevier]