Probing the anticancer activities of facial trioxorhenium and tricarbonylrhenium compounds with heterocyclic ligands.

The cytotoxicity of four rhenium compounds: fac-[ReO(impy)CH] (1) (impy = 2-(1H-imidazole-2-yl)pyridine), fac-[Re(CO)(bzimpy)Cl] (2) (bzimpy = 2-(2-pyridyl)benzimidazole), fac-[Re(CO)(bibzimpy)Cl] (3) (bibzimpy = 2,6-bis(2-benzimidazolyl)pyridine) and fac-[Re(CO)(impy)Cl] (4) was assessed against cancer cell lines, namely, the cervical hormone-responsive HeLa and the triple-negative breast cancer (TNBC) HCC70 lines versus a non-tumorigenic control breast epithelial cell line, MCF12A. A rare facial trioxorhenium(VII) compound 1 was characterized via various physicochemical techniques. The rhenium compounds 1-4 were, in general, more cytotoxic to HeLa cells, compared to the TNBC HCC70 line, displaying half maximal inhibitory concentration (IC) values in the micromolar range, however, the compounds were not convincingly selective for cancer cells over non-cancerous cells.

Anti-Amyloid Aggregation and Anti-Hyperglycemic Activities of Novel Ruthenium Uracil Schiff Base Compounds.

The formation and characterization of new diamagnetic ruthenium uracil mono-imine compounds: [(η-p-cymene)Ru(L)Cl][BF] (L=Hurpda=5-((pyridin-2-yl)methyleneamino)-6-aminouracil) for 1, urdpy=6-amino-1,3-dimethyl-5-((pyridin-2-ylmethylene)amino)uracil) for 2 or urqda=5-((quinolin-2-yl)methyleneamino)-6-aminouracil) for 3); cis-[Ru(bipy)(urpy)](BF) (4) (urpy=5-((pyridin-2-yl)methyleneamino)uracil) and cis-[Ru(bipy)(dapd)] (5) (Hdadp=5,6-diaminouracil) are described. A ruthenium(IV) uracil Schiff base compound, trans-[Ru(urpda)(PPh)Cl] (6) was also formed. Various physicochemical techniques were utilized to characterize the novel ruthenium compounds.

Bovine serum albumin uptake and polypeptide disaggregation studies of hypoglycemic ruthenium(II) uracil Schiff-base complexes.

Our prior studies have illustrated that the uracil ruthenium(II) diimino complex, [Ru(Hucp)Cl(PPh)] (1) (Hucp = 2,6-bis-((6-amino-1,3-dimethyluracilimino)methylene)pyridine) displayed high hypoglycemic effects in diet-induced diabetic rats. To rationalize the anti-diabetic effects of 1, three new derivatives have been prepared, cis-[Ru(bpy)(urdp)]Cl (2) (urdp = 2,6-bis-((uracilimino)methylene)pyridine), trans-[RuCl(PPh)(urdp)] (3), and cis-[Ru(bpy)(Hucp)](PF) (4). Various physicochemical techniques were utilized to characterize the structures of the novel ruthenium compounds.

Electrospun Nanofiber Composite Utilized as an Electrocatalyst for the Detection of Acetaminophen in Multifarious Water Samples.

Herein, the nanofabrication and characterization of new conductive materials, PANI-CoPc-fur () ((PANI = polyaniline and CoPc-fur = -4-(furan-2-methylthiophthalocyaninato)Co(II)) and PANI-CoPc-fur--MWCNTs () (-MWCNTs = carboxylic acid-functionalized multiwalled carbon nanotubes), are reported. Subsequently, an electrospun nanofiber (ENF) composite of , encapsulated with a poly(vinyl acetate) shell, was fabricated. The resultant core-shell nanoconjugated fibers, ENFs-, were adsorbed on a glassy carbon electrode (GCE), followed by the immobilization of a permeable adhesion top layer of Nafion (Nf) to render the chemically modified electrode, GCE|ENFs--Nf.

Ameliorative Effects of a Rhenium (V) Compound with Uracil-Derived Ligand Markers Associated with Hyperglycaemia-Induced Renal Dysfunction in Diet-Induced Prediabetic Rats.

Kidney disease is characterised by the improper functioning of the kidney as a result of kidney damage caused by hyperglycaemia-induced oxidative stress. The moderate hyperglycaemia seen in prediabetes can be treated using a combination of metformin and lifestyle interventions (low-calorie diets and exercising). However, patients have been reported to over-rely on pharmacological interventions, thus decreasing the efficacy of metformin, which leads to the development of type 2 diabetes mellitus (T2DM).

Biomolecular Interactions of Cytotoxic Ruthenium Compounds with Thiosemicarbazone or Benzothiazole Schiff Base Chelates.

Herein we illustrate the formation and characterization of new paramagnetic ruthenium compounds, trans-P-[RuCl(PPh ) (pmt)]Cl (1) (Hpmt=1-((pyridin-2-yl)methylene)thiosemicarbazide), trans-P-[RuCl(PPh ) (tmc)]Cl (2) (Htmc=1-((thiophen-2-yl)methylene)thiosemicarbazide) and a diamagnetic ruthenium complex, cis-Cl, trans-P-[RuCl (PPh ) (btm)] (3) (btm=2-((5-hydroxypentylimino)methyl)benzothiazole). Agarose gel electrophoresis experiments of the metal compounds illustrated dose-dependent binding to gDNA by 1-3, while methylene blue competition assays suggested that 1 and 2 are also DNA intercalators. Assessment of the effects of the compounds on topoisomerase function indicated that 1-3 are capable of inhibiting topoisomerase I activity in terms of the ability to nick supercoiled plasmid DNA.

Ruthenium compounds as potential therapeutic agents for type 2 diabetes mellitus.

Type 2 diabetes mellitus (T2DM) is a chronic metabolic disorder which is globally responsible for millions of fatalities per year. Management of T2DM typically involves orally administered anti-hyperglycaemic drugs in conjunction with dietary interventions. However, the current conventional therapy seems to be largely ineffective as patients continue to develop complications such as cardiovascular diseases, blindness and kidney failure.

Amelioration of risk factors associated with diabetic nephropathy in diet-induced pre-diabetic rats by an uracil-derived diimine ruthenium(II) compound.

Diabetic renal injury advances through different stages of structural and functional changes in the glomerulus, therefore treatment during the pre-diabetic state could be used as therapeutic target in the management and prevention of diabetic nephropathy (DN). Once diagnosed, dietary interventions and pharmacological therapy have been recommended to manage DN and pre-diabetic related complications. However, poor patient compliance still results, therefore newer alternative drugs are required.

Ruthenium complexes with or -heterocyclic chelates: DNA/BSA binding, antioxidant and anticancer studies.

Deoxyribonucleic acid (DNA) and bovine serum albumin (BSA) binding interactions for a series of ruthenium heterocyclic complexes were monitored using ultraviolet-visible (UV-Vis) spectrophotometry, fluorescence emission spectroscopy and agarose gel electrophoresis. Investigations of the DNA interactions for the metal complexes revealed that they are groove-binders with intrinsic binding constants in the order of 10 - 10 . Electronic spectrophotometric DNA titrations of the -heterocyclic metal complexes illustrated hypochromism of their intraligand electronic transitions and the presence of diffuse isosbestic points which are synonymous with homogeneous binding modes.

Hepatoprotective Effects of a Ruthenium(II) Schiff Base Complex in Rats with Diet-Induced Prediabetes.

Background: Progressive insulin resistance in a prediabetic state has been reported to be the predominant causative factor for the development of nonalcoholic fatty liver disease. The combination of dietary modification and pharmacotherapy has been recommended to manage diabetic liver complications. However, poor patient compliance and toxicity of current drug therapy on liver function still results; thus, newer alternative drugs are required.

DNA interaction studies of rhenium compounds with Schiff base chelates encompassing biologically relevant moieties.

Herein, we report the DNA interaction studies of rhenium(I) and -(V) compounds with Schiff base chelates encompassing biologically relevant moieties. More specifically, the DNA interaction capabilities of these rhenium complexes were probed using Gel Electrophoresis and Calf Thymus-DNA titrations monitored by temperature-controlled electronic spectroscopy. The DNA binding modes of the metal compounds were corroborated by molecular docking simulations.

Cardioprotective effects of a ruthenium (II) Schiff base complex in diet-induced prediabetic rats.

Background: Prediabetes and the onset of cardiovascular diseases (CVD) are strongly related. Prolonged hyperglycemia has been identified as a major contributing factor in the pathogenesis of CVD and diabetic complications. The management of hyperglycemia and prediabetes-associated vascular complications rely on pharmacotherapy and lifestyle intervention strategies.

Effects of a Ruthenium Schiff Base Complex on Glucose Homeostasis in Diet-Induced Pre-Diabetic Rats.

Pre-diabetes is a condition that precedes type 2 diabetes mellitus (T2DM) that is characterised by elevated glycated haemoglobin (HbA1c). The management of pre-diabetes includes the combination of dietary and pharmacological interventions to increase insulin sensitivity. However, poor patient compliance has been reported with regard to dietary interventions, therefore, new alternative drugs are required that can be effective even without the dietary intervention.

N-[(E)-Thio-phen-2-yl-methyl-idene]-1,3-benzothia-zol-2-amine.

In the title thio-phene-derived Schiff base compound, C(12)H(8)N(2)S(2), the thio-phene ring is slighty rotated from the benzothia-zole group mean plane, giving a dihedral angle of 12.87 (6)°. The largest displacement of an atom in the mol-ecule from the nine-atom mean plane defined by the non-H atoms of the benzothia-zole ring system is 0.

6-Amino-1,3-dimethyl-5-[(E)-2-(methyl-sulfan-yl)benzyl-idene-amino]-pyrimidine-2,4(1H,3H)-dione-1,3,7,9-tetra-methyl-pyrimido[5,4-g]pteridine-2,4,6,8-tetrone (1/1).

In the title co-crystal, C(12)H(12)N(6)O(4)·C(14)H(16)N(4)O(2)S, both mol-ecules are essentially planar [maximum deviations = 0.129 (1) and 0.097 (1) Å, respectively].