Amlexanox-modified platinum(IV) complex triggers apoptotic and autophagic bimodal death of cancer cells.

Platinum(IV) prodrugs c,c,t-[PtCl(NH)(OH)(amlexanox)] (MAP) and c,c,t-[PtCl(NH)(amlexanox)] (DAP) were synthesized by reacting amlexanox with oxoplatin and characterized by NMR, HR-MS, HPLC, and elemental analysis. The complexes could be reduced to platinum(II) species and amlexanox to exert antitumor activity. Generally, MAP was more potent than DAP and cisplatin towards various human cancer cell lines; particularly, it was active in cisplatin-resistant Caov-3 ovarian cancer and A549/DDP lung cancer cells.

Thiosemicarbazone N-Heterocyclic Cu(II) complexes inducing nuclei DNA and mitochondria damage in hepatocellular carcinoma cells.

The α-N-Heterocyclic thiosemicarbazones and their metal complexes have been widely investigated as anticancer and antibacterial agents for their broad spectrum of pharmacological properties. Thus, two thiosemicarbazone-based Cu(II) complexes, [Cu(ptpc)I] (1) and [Cu(qtpc)I] (2) with thiosemicarbazone ligand (ptpc = 2-(di(pyridin-2-yl)methylene)-N-(2-(trifluoromethyl)phenyl)-hydrazine-1-carbothioamide, qtpc = 2-(quinolin-8-ylmethylene)-N-(2-(trifluoromethyl)phenyl)hydrazine-1-carbothioamide) were synthesized and evaluated for their biological activities. Complexes 1 and 2 are superior to cisplatin in vitro antiproliferative activities toward hepatocellular carcinoma cell line with the half maximal inhibitory concentration value of 0.

Theoretical investigation into the cooperativity effect of 1,4-dimethoxy-D-glucosamine complex with Na and HO.

In order to explore the essence of the hydration process of chitin or chitosan in the presence of cation, the cooperativity effects between the H-bonding and Na···molecule interactions in the 1,4-dimethoxy-D-glucosamine (DMGA) complexes with HO and Na were investigated at the B3LYP/6-311++G(d,p), M06-2X/6-311++G(2df,2p), and ωB97X-D/6-311++G(2df,2p) levels. The result shows that the complexes in which Na or HO is bonded simultaneously to the -NH and -OH groups connected to the C3 atom of DMGA are the most stable. The cooperativity and anti-cooperativity effects occur in DMGA···HO···DMGA and DMGA···Na···HO, while only the cooperativities are confirmed in DMGA···Na···DMGA.

Influence of the introduction of a triphenylphosphine group on the anticancer activity of a copper complex.

Aiming at obtaining new copper complexes with good cytotoxicity against cancer cells, triphenylphosphine (TPP) was introduced to obtain insight into the influence of the co-ligands. In this paper, two copper complexes, Cu(2-pbmq)(CHOH)Br (1) and [Cu(2-pbmq)(TPP)Br] (2) were designed, synthesized, and characterized by X-ray crystallography, 2-((2-(pyrazin-2-yl)-1H-benzo[d]imidazol-1-yl)methyl))quinolone (2-pbmq), to investigate the influence of the TPP group on the anticancer activity of the metal complex. Although the presence of the TPP group diminished the intensity of the interaction properties of the complex with DNA, the in vitro anticancer activity and cellular uptake of the TPP-containing complex were markedly superior to those of its TPP-lacking counterpart.

Chemical biology suggests pleiotropic effects for a novel hexanuclear copper(ii) complex inducing apoptosis in hepatocellular carcinoma cells.

A novel hexanuclear copper(ii)-based complex, [Cu6(tpbb)2(NO3)12] (1), was synthesized, which shows potent cytotoxicity to hepatoma carcinoma cells by inducing apoptosis and apoptosis-related processes. Furthermore, mechanistic investigations based on proteomes revealed that the induced apoptosis was mediated by acting on several targets and multiple pathways in a pleiotropic way.

Synthesis and anticancer evaluation of benzo-N-heterocycles transition metal complexes against esophageal cancer cell lines.

Three novel transition metal complexes, Cu(p-2-bmq)Cl (1), Zn(p-2-bmq)Cl (2) and [Co(p-2-bmq)Cl] (3) (where p-2-bmq = 2-((1-(pyridin-2-yl)-1H-benzoimidazol-2-yl)methyl) quinolone, have been synthesized. The complexes were detected for their cytotoxicity in vitro against four human esophageal cancer cell lines (SMMC7721, BGC823, HCT116 and HT29) by MTT assay. The results showed that they all have anti-tumor cell proliferation activity.

Novel binuclear and trinuclear metal (II) complexes: DNA interactions and in vitro anticancer activity through apoptosis.

A water soluble trinuclear copper(II) complex and a binuclear cobalt(II) complex, namely Cu(ppbm)(SO) (1) and Co(ppbm)(NO) (2) (ppbm = 2-(pyridin-2-yl)-1-(pyridin-3-ylmethyl)- 1H-benzo[d]imidazole), have been successfully synthesized and characterized by elemental analysis, IR Spectroscopy, electrospray ionization mass spectra (ESI-MS). The interaction of the new complexes with DNA has been explored using spectroscopy methods, indicating that the complexes 1 and 2 bind to DNA via noncovalent interactions. DNA cleavage experiment suggested that the complex 1 exhibits efficient DNA cleavage activities in the presence of ascorbate (Asc), hydrogen peroxide may serve as the major cleavage active species.

Quartz filter-based thermal desorption gas chromatography mass spectrometry for in-situ molecular level measurement of ambient organic aerosols.

Thermal desorption aerosol gas chromatography (TAG) is an effective technique for online chemical characterization of organics in atmospheric fine particulate matter (PM) on the molecular level. Unlike the previously reported impactor- or metal filter-based TAG, in this study, a replaceable quartz filter-based TAG (Q-TAG) was developed to achieve online measurement of organic constituents in ambient PM. A homemade device for automatic online sampling and pretreatment of aerosols was developed and coupled with gas chromatography-mass spectrometry (GC-MS) by a 4-port valve.

DNA interactions and anticancer evaluations of pyridine-benzimidazole-based Cu complexes.

Copper is an essential element and has redox potential, thus copper complexes have been developed rapidly with the hope of curing cancer. To further develop anticancer agents and investigate their anticancer mechanisms, two Cu complexes, [Cu(bpbb)·Cl·SCN]·(CHOH) () and [Cu(bpbb)·Br·(OH)] (), were synthesized and characterized using 4,4'-bis((2-(pyridin-2-yl)-1-benzo[]imidazol-1-yl)methyl)biphenyl (bpbb), with associated Cu(ii) salts. Complex is a binuclear structure, whereas is a one-dimensional complex.

Cytotoxicity, dual-targeting apoptosis induction evaluation of multinuclear cu complexes based on pyrazine-benzimidazole derivative.

To investigate the cytotoxicity and mechanism of action of multinuclear Cu complexes against tumor cell lines, two complexes, Cu(bpbib)Br (1) and Cu(bpbib)(BF)Cl (2) (bpbib = 1,4-bis((2-(pyrazin-2-yl)-1H-benzo[d]imidazol-1-yl)methyl)benzene) were synthesized and characterized. Both Cu complexes showed high selectivity toward cancer and not normal cells, and the SMMC7721 cell line showed most sensitivity toward both complexes. Complex 1 exhibited more potent cytotoxicity and enhanced cellular uptake, and therefore, was comprehensively investigated.

In vitro antitumor activity of novel benzimidazole-based Cu(II) complexes.

Four benzimidazole-based Cu(II) complexes: Cu(p-2-bmp)Br (1), Cu(p-2-bmp)Cl (2), Cu(p-2-bmb)(DMF)Br·(CHCl) (3), and Cu(p-2-bmb)(NO)·(CHCl) (4) were isolated and characterized, where p-2-bmp is 1-((2-(pyridine-2-yl)-1H-benzoimidazol-1-yl)methyl)-1H-pyridine and p-2-bmb is 1-((2-(pyridin-2-yl)-1-benzoimidazol-1-yl)methyl)-1H-benzotriazole. Complexes 1 and 2 have binuclear configurations, 3 has a mononuclear structure, and 4has a one-dimensional (1-D) chain skeleton. To evaluate their potential anticancer effects on human carcinoma cells, anti-proliferation, DNA binding and cleavage, and apoptosis elicitation were examined.

miR‑140‑5p inhibits human glioma cell growth and invasion by targeting JAG1.

miR‑140‑5p has been reported to be a tumor suppressor in several types of human cancer, however, little is known about its expression and function in human gliomas. The present study aimed to detect the expression of miR‑140‑5p in human glioma tissues and cell lines, and to investigate the effect of miR‑140‑5p on glioma cell growth, invasion and adhesion using in vitro gain‑of‑function and loss‑of‑function experiments. Furthermore, the hypothesis that Jagged1 (JAG1) may be a target gene of miR‑140‑5p was tested.

Feasibility and safety of prophylactic tentorium cerebelli hiatus incision in surgery of glioma located in lateral fissure area.

To discuss the feasibility and safety of prophylactic tentorium cerebelli hiatus incision in surgery of glioma located in lateral fissure area. There were 80 patients with glioma located in lateral fissure area who received treatment from May 2012 to May 2015, divided into two groups, the research group (n=40) and control group (n=40), and then statistical analysis was carried out. Difference in total resection rate and subtotal resection rate of glioma between patients of the research group and those of the control group was not significant (P>0.

Bis{μ-1,3-bis-[(2-methyl-1H-benzimid-azol-1-yl)meth-yl]benzene-κN:N}bis-(diiodidocadmium).

In the title compound, [Cd(2)I(4)(C(24)H(22)N(4))(2)], the 1,3-bis-[(2-methyl-1H-benzimidazol-1-yl)meth-yl]benzene ligand bridges two CdI(2) units, forming a centrosymmetric dinuclear complex. The Cd(II) atom adopts a distorted tetra-hedral coordination geometry. In the crystal, complex mol-ecules are linked into columns parallel to [101] by π-π stacking inter-actions, with centroid-centroid distances of 3.

Construction of a Ag(12) high-nuclearity metallamacrocyclic 3D framework.

An unprecedented high-nuclearity metallamacrocycle-based 3D silver framework with formula {[Ag(2)(C(25)H(27)N(6)O)(2)](CH(3)OH)(H(2)O)(0.17)}(n) (1), built on the basis of dodecanuclear silver building blocks, has been synthesized and characterized, and it shows strong phosphorescence emission at 10 K, which is a consequence of the presence of intersystem crossing from singlet to triplet caused by the heavy-atom effect of silver ions.

Cation exchange induced tunable properties of a nanoporous octanuclear Cu(II) wheel with double-helical structure.

A double-helical octanuclear Cu(II) wheel 1 with 2.88 nm diameter was prepared through the reaction of a clinical medicine, telmisartan, with copper sulfate. Central copper ions can be partially replaced by bivalent zinc and cobalt ions and fully exchanged by trivalent iron ions.