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A dioxovanadium(V) complex, [VO2(moptpy)](ClO4) (1, moptpy = 4′-(3-methoxyphenyl)2,2′:6′2″-terpyridine), was synthesized and characterized by elemental analysis, ESI-MS, UV–vis, IR, and1H,13C, and51V NMR. The cytotoxicityin vitroof1was evaluated against cancer cell lines HepG-2 (hepatocellular carcinoma), SGC-7901 (gastric carcinoma), SiHa (cervical cancer), BEL-7402 (hepatocellular), and rat PC-12 (pheochromocytoma) by the MTT method. The results demonstrated that1exhibits superior anticancer activityin vitrowith much lower values of 50% inhibitive concentration (IC50) against the selected cell lines than cisplatin, and1shows the highest cytotoxic activity toward SGC-7901 cells (IC50 = 1.3 ± 0.1 μM) among the selected cell lines. A series of cellular morphological and staining experiments were carried out, and the results indicated that1can effectively induce apoptosis of SGC-7901 cells through a ROS-mediated mitochondrial dysfunction pathway. In addition, cellular incorporation and cell cycle analysis were also performed, and it was concluded from the experimental observations that1can efficiently enter into the cell nuclei, and the complex inhibits cell growth in SGC-7901 cell at G0/G1 phase. [ABSTRACT FROM AUTHOR]

We report herein the identification of an immunomodulatory metal-based complex 1 as a direct inhibitor of TLR1/2 heterodimerization. Both enantiomers of complex 1 selectively suppressed TNF-α and TLR1/2 heterodimerization in Pam3CSK4-induced macrophages, with Λ-1 being more potent than Δ-1. Moreover, the complexes inhibited NF-κB transduction via the modulation of TLR1/2 signaling. To our knowledge, complex 1 is the first metal-based inhibitor of TLR1/2 heterodimerization reported to date. [ABSTRACT FROM AUTHOR]

A novel luminescent cyclometalated iridium(iii) complex 1 was synthesized and employed as a chemosensor for the detection of Al3+ ions. Compared with common organic chemosensors, 1 displays a larger Stokes shift and a long lifetime luminescence that allow 1 to detect Al3+ ions in fluorescent dye spiked strong fluorescence media and potentially be used in strongly autofluorescent biological samples. [ABSTRACT FROM AUTHOR]

We report herein a novel iridium(iii) complex 1 as an antitumour necrosis factor agent and the first metal-based inhibitor of TACE enzymatic activity. Complex 1 inhibited TNF-α secretion and p38 phosphorylation in human monocytic THP-1 cells. [ABSTRACT FROM AUTHOR]

Metal-containing complexes have arisen as viable alternatives to organic molecules as therapeutic agents. Metal complexes possess a number of advantages compared to conventional carbon-based compounds, such as distinct geometries, interesting electronic properties, variable oxidation states and the ability to arrange different ligands around the metal centre in a precise fashion. Meanwhile, nitric oxide (NO) plays key roles in the regulation of angiogenesis, vascular permeability and inflammation. We herein report a novel cyclometalated rhodium(III) complex as an inhibitor of lipopolysaccharides (LPS)-induced NO production in RAW264.7 macrophages. Experiments suggested that the inhibition of NO production in cells by complex 1 was mediated through the down-regulation of nuclear factor-κB (NF-κB) activity. Furthermore, complex 1 inhibited angiogenesis in human umbilical vein endothelial cells (HUVECs) as revealed by an endothelial tube formation assay. This study demonstrates that kinetically inert rhodium(III) complexes may be potentially developed as effective anti-angiogenic agents. [ABSTRACT FROM AUTHOR]

Kinetically inert metal complexes have arisen as promising alternatives to existing platinum and ruthenium chemotherapeutics. Reported herein, to our knowledge, is the first example of a substitutionally inert, Group 9 organometallic compound as a direct inhibitor of signal transducer and activator of transcription 3 (STAT3) dimerization. From a series of cyclometalated rhodium(III) and iridium(III) complexes, a rhodium(III) complex emerged as a potent inhibitor of STAT3 that targeted the SH2 domain and inhibited STAT3 phosphorylation and dimerization. Significantly, the complex exhibited potent anti-tumor activities in an in vivo mouse xenograft model of melanoma. This study demonstrates that rhodium complexes may be developed as effective STAT3 inhibitors with potent anti-tumor activity. [ABSTRACT FROM AUTHOR]

We report herein a novel luminescent iridium(III) complex with two hydrophobic carbon chains as a non-reaction based chemosensor for the detection of Hg2+ ions in aqueous solution (<0.002% of organic solvent attributed to the probe solution). Upon the addition of Hg2+ ions, the emission intensity of the complex was significantly enhanced and this change could be monitored by the naked eye under UV irradiation. The iridium(III) complex shows high specificity for Hg2+ ions over eighteen other cations. The system is capable of detecting micromolar levels of Hg2+ ions, which is within the range of many chemical systems. [ABSTRACT FROM AUTHOR]

Highlights: [•] Transcription factors have emerged as promising therapeutic targets for a variety of human diseases. [•] Examples of metal complexes that inhibit transcription factor activity are highlighted. [•] Modes of action include binding to transcription factors, binding to DNA, or inhibiting upstream targets. [ABSTRACT FROM AUTHOR]

Highlights: [•] A luminescent probe for human serum albumin in aqueous solution has been developed. [•] A novel luminescence switch-on iridium(III) complex is reported. [•] The assay is selective for human serum albumin. [Copyright &y& Elsevier]