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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]

Six new gold(III) complexes [Au(bzpam)Cl2] (1, bzpamH = N-benzyl picolinamide), [Au(hetpam)Cl2] (2, hetpamH = N-(2-hydroxyethyl) picolinamide), [Au(pypam)Cl]AuCl4 (3, pypamH = N-(pyridin-2-ylmethyl) picolinamide), [Au(dmepam)Cl]AuCl4 (4, dmepamH = N-(2-(dimethylamino)ethyl) picolinamide), [Au(bhetpydam)Cl] (5, bhetpydamH2 = N,N′-bis(2-hydroxyethyl) pyridine- 2,6-dicarboxamide) and [Au2(hedam)Cl4] (6, hedamH2 = N, N′-(hexane-1,6-diyl) dipicolinamide) with deprotonated pyridyl carboxamide were synthesized and characterized by elemental analysis, molar conductivity, IR, H1 NMR and C13 NMR techniques. The analytical data showed that deprotonated pyridyl carboxamide coordinated with gold(III) ions through a nitrogen atom. The cytotoxicity against Bel-7402 and HL-60 cell lines was tested by MTT (3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) and SRB (sulforhodamine B) assays. The results indicated that the complexes exerted cytotoxic effects against Bel-7402 and HL-60 cell lines, complex 6 had better cytotoxicity than cisplatin, and complex 3 displayed similar cytotoxicity to cisplatin against Bel-7402 cell line. The results suggested that the characteristics of ligands had an important effect on cytotoxicity of complexes. Copyright © 2012 John Wiley & Sons, Ltd. [ABSTRACT FROM AUTHOR]

Eight new palladium(II) complexes with 4-toluenesulfonyl-L-amino acid dianion and 1,4-dab/1,3-dap, [Pd(1,4-dab)(TsglyNO)] · H2O (1), [Pd(1,4-dab)(TsvalNO)] (2), [Pd(1,4-dab)(TsleuNO)] (3), [Pd(1,4-dab)(TsileNO)] (4), [Pd(1,4-dab)(TsserNO)] · 0.5H2O (5), [Pd(1,4-dab)(TspheNO)] · 0.5H2O (6), [Pd(1,4-dab)(TsthrNO)] · H2O (7), and [Pd(1,3-dap)(TsserNO)] (8), have been synthesized and characterized by elemental analysis, IR, UV, 1H NMR, and mass spectrometry. Crystal structure of 8 has been determined by X-ray diffraction. The cytotoxicities were tested by MTT assay. The results indicate the complexes exert cytotoxic effects against HL-60 and Bel-7402. The structure–activity relationship suggests that both amino acids and N-containing ligands have important effects on cytotoxicity, but the IC50 values do not show definite correlation with variation of these ligands. [ABSTRACT FROM PUBLISHER]

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]

Abstract: Six new mixed ammine/ethylamine platinum(II) complexes with carboxylates [Pt(II)(NH3)(C2H5NH2)X2] (a–f) (X=CH3COO−, CH2ClCOO−, C6H5–COO−, p-CH3–C6H4–COO−, p-CH3O–C6H4–COO−, p-NO2–C6H4–COO−) (a–f) have been synthesized and characterized by elemental analysis, conductivity, spectra techniques (IR, UV and 1H NMR). The cytotoxicity of the complexes was tested by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay. The relative reactivity of leaving groups of complex (c) with G-actin was determined spectrophotometrically at 412nm. The results show that the complexes (a–f) confer substantially greater cytotoxicity against EJ and HL-60 than the other carcinoma cell lines, moreover, the cytotoxicity of complexes (c–e) is equal to that of cisplatin against HL-60, and the cytotoxicity of complex (c) is also equal to that of cisplatin against EJ. However the complexes (a–f) are significantly less potent than cisplatin against BGC-823, HCT-8 and MCF-7. The reactivity of leaving groups decreases in the sequence: cisplatin> c >carboplatin. The results suggest that ammine/ethylamine platinum(II) complexes with carboxylate anion as leaving group have selectivity against carcinoma cell lines. When leaving group is aromatic carboxylate ion, the complexes have better cytotoxicity, moreover, the substitution radical in benzene ring also influences cytotoxicity. [Copyright &y& Elsevier]

Abstract: Five new type binuclear platinum(II) complexes (a–e) have been synthesized and characterized by elemental analysis, conductivity, thermal analysis, IR, UV, 1H NMR and mass spectral techniques. The cytotoxicity of the complexes was tested by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) and sulforhodamine B (SRB) assays. The acute toxicity and antitumor activity of complex e in vivo were also studied. The results indicate that complexes a–d have no activity against HL-60, MCF-7, BGC-823, EJ and HCT-8 cell lines, with a higher IC50 value (>50μM). Complex e confers substantially greater cytotoxicity against HL-60, MCF-7, BGC-823, EJ and HCT-8 cell lines with an IC50 value of 0.02±0.009, 1.70±0.21, 4.00±0.35, 0.98±0.02 and 1.02±0.21μM, respectively. LD50 of complex e is 815.3mg/kg, it was significantly higher than that of cisplatin and carboplatin. Complex e at dose of 4, 12 and 20mg/kg has no activity against mouse hepatocarcinoma H22 and Lewis lung carcinoma in mice, but displays significant activity against human ovarian carcinoma A2780 and human colon carcinoma HCT-116 in nude mice at dose of 12mg/kg, and activity is similar to that of cisplatin at dose of 4mg/kg. Complex e at dose of 20mg/kg has no activity against human lung adenocarcinoma A549 in nude mice (P >0.05). The results suggest that the species of amine for the new type binuclear platinum complexes have important effect on their cytotoxicity, and they may be a new class platinum anticancer drugs. [Copyright &y& Elsevier]

Seven flavonol glycosides and four nonflavonoid compounds were isolated from Epimedium koreanum Nakai (Berberidaceae), and their effects on the proliferation of rat osteoblast-like (ROB) cells were evaluated with a mitochondrial activity assay. Both flavonol glycosides and nonflavonoid compounds strongly inhibited the proliferation of primary ROB cells at most concentrations (2.0 × 10- 5 mol/L ∼ 1.0 × 10-8 mol/L), and a simple structure-function relationship was also found in these compounds. Considering the antiosteoporotic effect of flavonoids in vivo, these results suggest that the flavonoids may enhance the development of osteoblasts through their active metabolites, and the mechanism between proliferation and differentiation of osteoblasts needs to be further studied to fully evaluate the mechanism of E. koreanum in the treatment of osteoporosis. [ABSTRACT FROM AUTHOR]

Abstract: Seven new tri-functional mononuclear platinum(II) complexes (a–g) have been synthesized and characterized by elemental analysis, conductivity, thermal analysis, IR, UV and 1H NMR spectral techniques. The cytotoxicity of these 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. The results indicate that the complexes (a–g) have selectivity against tested carcinoma cell lines; they have weaker cytotoxicity against HCT-8 and MCF-7. Complexes a, b, d and g also exert weaker cytotoxicity against BGC-823 and complexes a, b, e and f have better cytotoxicity against EJ, but their cytotoxicity is weaker than that of cisplatin. Complexes c, e and f, confer substantially greater cytotoxicity against HL-60 with an IC50 value of 7.68±0.23, 3.87±0.19 and 2.41±0.18μM, respectively, moreover, cytotoxicity of complex f is equal to that of cisplatin. Complexes c, e and f cause significant G2/M arrest and a concomitant decrease of cell population in G1 and S phases. The total DNA-platination levels of them are higher than that of cisplatin under the same experimental conditions. It suggests that there is no correlation between total DNA-platination levels in HL-60 cells and cytotoxicity of complexes. When leaving groups are aromatic carboxylates, the complexes have better cytotoxicity, moreover, the substituent in benzene ring also influences cytotoxicity. In addition, when leaving groups are dicarboxylates, dicarboxylates coordinating with platinum through oxygen atoms form different chelate cycle and cycle size also affects their cytotoxicity. [Copyright &y& Elsevier]

Abstract: Seven new mixed ammine/propylamine platinum(II) complexes with carboxylates (a–g) have been synthesized and characterized by elemental analysis, conductivity, IR, UV, and 1H NMR spectra techniques. The cytotoxicity of these complexes was tested by MTT assay. The levels of total platinum bound to DNA were measured by ICP-MS. The results indicate that the complexes (a–g) have better cytotoxicity against EJ and HL-60 than other carcinoma cell lines. The cytotoxicity increases in the sequence: g < f < e < d < b < c < a against tested carcinoma cell lines. The cytotoxicity of complexes (a–c) is equal to that of cisplatin against HL-60. The cytotoxicity of complex a is also equal to that of cisplatin against EJ. However, the complexes (a–g) are significantly less potent than cisplatin against BGC-823, HCT-8 and MCF-7. The total DNA-platination levels increase in the sequence: cisplatin

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]

Ten novel palladium(II) complexes with dipyrido[3,2- d :2′,3′- f ]quinoxaline (Dpq)/dipyrido[3,2- a :2′,3′- c ](6,7,8,9-tetrahydro)phenazine (Dpqc) and 4-toluensulfonyl- L -amino acid dianion, [Pd(Dpq)(TsvalNO)]·H 2 O ( 1a ), [Pd(Dpq)(TsileNO)]·H 2 O ( 1b ), [Pd(Dpq)(TsserNO)] ( 1c ), [Pd(Dpq)(TsthrNO)]·1.5H 2 O ( 1d ), [Pd(Dpq)(TsleuNO)]·0.5H 2 O ( 1e ), [Pd(Dpq)(TspheNO)] ( 1f ), [Pd(Dpqc)(TsvalNO)] ( 2a ), [Pd(Dpqc)(TsileNO)] ( 2b ), [Pd(Dpqc)(TsserNO)]·H 2 O ( 2c ) and [Pd(Dpqc)(TsthrNO)]·0.5H 2 O ( 2d ) have been synthesized and characterized by elemental analysis, IR, UV, 1 H NMR and mass spectrometry techniques. Crystal structure of the complex 1f has been determined by X-ray diffraction. The cytotoxicity was tested by MTT assay. The results indicated that the complexes 1a and 2a showed better cytotoxicity than cisplatin against MCF-7. The complex 1e had higher cytotoxicity than cisplatin against K562. Both the N donating ligands and the amino acid have important effects on the cytotoxicity. [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: Seven new Au(III) complexes ([(PipDTC)AuCl2] (1), [(MoDTC)AuCl2] (2), [(BzoPizDTC)AuCl2] (3), [(TsPizDTC)AuCl2] (4), [(PizDTC)Au2Cl4] (5), [(MePizDTC)Au2Cl5] (6) and [(EtPizDTC)Au2Cl5] (7)) with cyclic amine-based dithiocarbamate have been synthesized, characterized and evaluated in vitro. The results indicate that these complexes exert selective cytotoxic effects against HL-60, BGC-823, Bel-7402 and KB cells lines. Complex 1 shows 11-, 5- and 1-folds higher cytotoxicity than cisplatin against KB, BGC-823 and Bel-7402 cell lines. Complex 2 exhibits higher cytotoxicity than cisplatin against BGC-823 and Bel-7402 cell lines. Complexes 3 and 4 display higher cytotoxicity than cisplatin against BGC-823 cell line. The nature of cyclic amine and the number of metal centers have important effects on cytotoxicity of these Au(III) complexes. [Copyright &y& Elsevier]

Abstract: A series of phenanthrene imidazole with polyglycol side chain (2a–2c and 3a–3c) were synthesized and characterized by IR, NMR and MS. The cytotoxicity of 2a–2c and 3a–3c against cancer cell lines (HL-60, BGC-823, Bel-7402 and KB) in vitro were measured using MTT method. The DNA binding properties of 3a–3c were investigated by UV, fluorescence, CD spectroscopies and thermal denaturation. The results indicate that 2a exhibits higher cytotoxicity than cisplatin against BGC-823 and Bel-7402 cell lines, 3b and 3c exhibit higher cytotoxicity than 2b and 2c against BGC-823, Bel-7402 and KB cell lines. The cytotoxic effect of 2a–2c decrease with the increase of side chains length, the cytotoxic effect of 3a–3c increased with the increasing length of side chains against BGC-823, Bel-7402 and KB cell lines. Compounds 3a–3c intercalated DNA with a vertical orientation in the intercalation pocket. The binding constants of 3a–3c with Ct-DNA are 1.68×106, 1.51×106 and 0.709×106 M−1, respectively. The binding affinity of 3a–3c with Ct-DNA trended to decrease with the increasing length of polyglycol side chains. [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]