Click synthesis, anticancer activity, and molecular docking investigation of some functional 1,2,3-triazole derivatives

1,2,3-triazole skeleton is a privileged building block for the discovery of new promising anticancer agents. In this report, new 1,4-disubstituted 1,2,3-triazoles with the bioisoster triazole moiety were straightforwardly prepared under copper-catalyzed azide-alkyne [3+2] cycloaddition reactions (CuAAC) regime using a variety of both functional organic azides and terminal alkynes. The resulting functional 1,4-disubstituted 1,2,3-triazole compounds were fully characterized and subsequently tested for their antiproliferative activity against four different cancer cell lines. The cytotoxicity tests carried out with these 1,2,3-triazole derivatives show average IC50 values ranging from 15 to 50 μM by comparison with the standard reference drug, namely doxorubicin. The phosphonate 1,2,3-triazole derivative was found to exhibit the best antiproliferative activity among the studied compounds against the HT-1080 cell lines. It was chosen to evaluate its mode of action in these cancer cell lines. The cell cycle study showed that the phosphonate derivative, compound 8, is the most active inhibitor of the cell cycle at the G0/G1 phase, inducing apoptosis independently of Caspase-3 and causing an increase in the mitochondrial membrane potential (ΔΨm) in the HT-1080 cell lines. Molecular docking studies of this phosphonate derivative into the MMP-2 and MMP-9 metalloproteinases receptors demonstrated the relevance of triazole scaffolds and the pendant phosphonate group in establishing -anion, -alkyl and hydrogen bonding type interactions with residual components in the active MMP pocket

CONTRIBUTION A L’ETUDE DE L’INHIBITION DE LA CORROSION DU FER PAR LE MONOFLUOROPHOSPHATE DE MANGANESE

The inhibiting effect of manganesemonofluorophosphate on the ironcorrosion in 3% NaCl solution wasinvestigated using electrochemicalimpedance spectroscopy. Anequivalent circuit is assumed in orderto characterize the film capacitance, the charge transfer resistance at the interface and the ionic flux across the film. The infrared reflection spectroscopy (IRRAS) revealed the presence of monofluorophosphate group on the electrode surface and other iron species.L'effet inhibiteur du monofluorophosphate de manganèse sur la corrosion du fer dans le milieu NaCl 3% a été étudié par spectroscopie d'impédance électrochimique. Un circuit équivalent est utilisé pour caractériser la capacité de film, la résistance de transfert de charge à l'interface et le flux ionique à travers le film. La spectroscopie infrarouge à transformée de Fourrier (IRRAS) a indiqué la présence du groupement monofluorophosphate à la surface de l’électrode de fer et d’autres espèces à base du fer

Adsorptive removal of anionic dye from aqueous solutions using powdered and calcined vegetables wastes as low-cost adsorbent

In this study, we describe a behaviour comparison between powdered and calcined adsorbents prepared from vegetables waste of Persea species to remove Eriochrome Black T as anionic dye from aqueous solutions. Potential capabilities of these two adsorbents have been evaluated by studying some experimental parameters such as solution pH, adsorbent dosage, initial dye concentration, contact time and temperature. Kinetic study has been achieved by the application of pseudo-first and second orders and Elovich model. Results found agreed well with the pseudo-second order model. The experimental data were analysed using Langmuir, Freundlich and Tempkin isotherms models. The equilibrium data fitted well with the Freundlich isotherm and the adsorption capacities were calculated to be 120.50 mg/g and of 96.15 mg/g for calcined and powdered adsorbents, respectively. Thermodynamic study was also undertaken and provided important results indicating a spontaneous reaction and feasibility on the two adsorbents. The two adsorbents have been characterized via spectroscopic data such infrared spectrum, X-ray and by emission scanning electron microscopy

Etude de l’inhibition de la corrosion du fer en milieu sulfurique 1 M par l’acide hexa méthylène diamine tétra méthyle phosphonique

The efficiency of hexa methylene diamine tetra methyl-phosphonic acid (HMDTMP), as corrosion inhibitor for iron in 1M H2SO4, has been determined by gravimetric and electrochemical measurements. Polarization curves indicate that the compound is mixed inhibitor, affecting both cathodic and anodic corrosion currents. Adsorption of HMDTMP derivatives on iron surface is in agreement with the Langmuir adsorption isotherm model, and the calculated Gibbs free energy value confirms the chemical nature of the adsorption. EIS results show that the change in the impedance parameters (Rt and Cdl) with concentration of HMDTMP is indicative. The adsorption of this molecule leads to the formation of a protective layer on iron surface.L'effet inhibiteur de l’acide hexaméthylène diamine tétra méthylène phosphonique (HMDTMP) sur la corrosion du fer en milieu H2SO4 1M a été étudié à l'aide des méthodes électrochimiques et gravimétriques. Les courbes de polarisation indiquent que le composé est un inhibiteur mixte, réduisant à la fois les courants de corrosion cathodique et anodique. L’adsorption de HMDTMP à la surface du fer suit l’isotherme du modèle de Langmuir, et la valeur obtenue de l’énergie libre de Gibbs confirme la nature chimique de l'adsorption. Les mesures d’impédance électrochimiques montrent que la variation des paramètres d'impédance (Rt et Cdl) avec la concentration de HMDTMP est indicative. L'adsorption de cette molécule conduit à la formation d'une couche protectrice sur la surface du fer

The potential use of activated carbon prepared from Ziziphus species for removing dyes from waste waters

Abstract In this study, the adsorption potential of activated carbon prepared from Ziziphus mauritiana nuts for the removal of methylene blue (MB) from aqueous solution has been investigated using batch mode experiments. The effects of some operating parameters on the removal dye such as, initial pH (2–12), temperature (298–328 K), initial MB concentration (20–100 mg L−1), and contact time (5–70 min) were investigated. Adsorption kinetic showed that the rate adsorption followed the pseudo-second-order kinetic model. Four adsorption isotherms models were applied to experimental equilibrium data (Langmuir, Freundlich, Redlich–Peterson, and Fritz–Schlunder) and the different constants were calculated using non-linear equations models. Fritz–Schlunder model was found the best one to describe the adsorption process which suggests that the adsorption of MB onto activated carbon derived from Ziziphus mauritiana is heterogeneous with a multilayer. Thermodynamic adsorption showed that the process was endothermic and spontaneous in nature

An Overview on the Performance of 1,2,3-Triazole Derivatives as Corrosion Inhibitors for Metal Surfaces

This review accounts for the most recent and significant research results from the literature on the design and synthesis of 1,2,3-triazole compounds and their usefulness as molecular well-defined corrosion inhibitors for steels, copper, iron, aluminum, and their alloys in several aggressive media. Of particular interest are the 1,4-disubstituted 1,2,3-triazole derivatives prepared in a regioselective manner under copper-catalyzed azide-alkyne cycloaddition (CuAAC) click reactions. They are easily and straightforwardly prepared compounds, non-toxic, environmentally friendly, and stable products to the hydrolysis under acidic conditions. Moreover, they have shown a good efficiency as corrosion inhibitors for metals and their alloys in different acidic media. The inhibition efficiencies (IEs) are evaluated from electrochemical impedance spectroscopy (EIS) parameters with different concentrations and environmental conditions. Mechanistic aspects of the 1,2,3-triazoles mediated corrosion inhibition in metals and metal alloy materials are also overviewed