Anti-cancer,anti-oxidant and molecular docking studies of thiosemicarbazone indole-based derivatives

Based on the structural elements of bioactive 3-substituted indoles, a new series of indole–thiosemicarbazone hybrid derivatives were designed, synthesized, and well-characterized using different spectral techniques. The intended scaffolds were screened for their in vitro anti-proliferative activities against breast cancer (MCF-7), lung cancer (A-549), and liver cancer (Hep-G2) cell lines, as well as their anti-oxidant properties. Cytotoxicity studies revealed that compound 6n was the most potent, at least threefold more potent than the commercially available reference drug etoposide, against A-549. In addition, morphological analysis by the acridine orange/ethidium bromide double staining test and flow cytometry analysis confirmed induction of apoptosis in the A-549 cells by compound 6n. In order to validate the experimental results, molecular studies were performed to achieve the possible binding interactions of the most potent compound (6n) and colchicine with tubulin as well as ANP with ATPase domain of topoisomerase IIα active sites. Moreover, the radical scavenging potential of the final derivatives was found to be excellent with the range of 0.015–0.630 µM, comparable to the standard ascorbic acid (0.655 µM).

     

Design and synthesis of 2,4-dioxochroman-pyridinium-phenylacetamide derivatives as new anti-Alzheimer agents: in vitro and in silico studies

2,4-Dioxochroman-pyridinium-phenylacetamide derivatives 7a–n were synthesized and evaluated for their in vitro cholinesterase (ChE) inhibitory activities against acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). Obtained results demonstrated that, among the synthesized compounds, two compounds, 7j and 7k , were more potent than the standard drug donepezil against BuChE and did not show cytotoxicity and carcinogenicity. Furthermore, through molecular modeling and molecular dynamic studies. we showed that these compounds can be located deep in the gorge cavity of BuChE and that they interacted with catalytic residues, acyl, and cholin-binding pockets of this enzyme. Support information     

Highly stable electrochemical oxidation of phenolic compounds at carbon ionic liquid electrode

A carbon ionic liquid electrode (CILE) was used for the investigation of the electrochemical oxidation of phenolic compounds in acidic media using cyclic voltammetry, chronoamperometry and square wave voltammetry techniques. The results indicate that, contrary to many other electrodes, the oxidation of phenolic compounds on CILE is highly stable and does not result in electrode fouling. Cyclic voltammetry showed that phenolic compounds such as phenol, 2,4-dichlorophenol and catechol were oxidized at CILE and remained electroactive after multiple cycles and at high concentrations of phenol. The cyclic voltammetric response of the CILE is very stable with more than 99% of the initial activity remaining after 20 s of stirring of a 0.5 mM solution of phenol.     

Ultra trace adsorptive stripping voltammetric determination of atrazine in soil and water using mercury film electrode

In situ mercury film electrode produced in the presence of thiocyanate has been shown extremely useful for highly sensitive adsorptive stripping voltammetric measurements of atrazine down to sub-μg L⁻¹ level. Operational parameters have been optimized and the stripping voltammetric performance has been investigated using square wave scans. The adsorptive stripping response is linear over the range of 0.5-60 μg L⁻¹ atrazine, with a detection limit of 0.024 μg L⁻¹. The method has been applied to the determination of atrazine in soil and water samples.     

Synthesis and Characterization of Nickel Oxide Nanoparticles from Ni(salen) as Precursor

Nickel oxide nanoparticles have been synthesized by thermal treatment of N,N′-(bis(salicylidene)-ethylene-1,2-diamine)Nickel(II); [Ni(salen)]; as precursor which has been synthesized via two methods: [Ni(salen)] were obtained by solid state reaction in absence solvent and co-precipitation reaction in presence of propanol as solvent, respectively. Nickel oxide nanoparticles were characterized by X-ray diffraction, scanning electron microscopy, transmission electron microscopy and Fourier transform infrared spectroscopy.     

Construction of a carbon nanocomposite electrode based on amino acids functionalized gold nanoparticles for trace electrochemical detection of mercury

A simple, highly sensitive and selective carbon nanocomposite electrode has been developed for the electrochemical trace determination of mercury. This mercury nanocomposite sensor was designed by incorporation of thiolated amino acids capped AuNps into the carbon ionic liquid electrode (CILE) which provides remarkably improved sensitivity and selectivity for the electrochemical stripping assay of Hg(II). Mercury ions are expected to interact with amino acids through cooperative metal–ligand interaction to form a stable complex which provides a sensitive approach for electrochemical detection of Hg(II) in the presence of other metal ions. The detection limit was found to be 2.3 nM (S/N = 3) that is lower than the permitted value of Hg(II) reported by the Environmental Protection Agency (EPA) limit of Hg(II) for drinkable water. The proposed nanocomposite electrode exhibits good applicability for monitoring Hg(II) in tap and waste water.     

Voltammetric Determination of Hemoglobin Using a Pencil Lead Electrode

In this paper the electrochemical behavior of hemoglobin (Hb) immobilized on a pencil lead electrode (PLE) was investigated. Immobilization of Hb on the pencil lead electrode was performed by nonelectrochemical and electrochemical methods. In phosphate buffer solution with pH 7.0 Hb showed a pair of well‐defined and nearly reversible redox waves (the anodic and cathodic peak potentials are located at ?0.18 V and ?0.22 V, respectively). The dependence of the anodic peak potential (E_pa) on the pH of the buffer solution indicated that the conversion of Hb? Fe(III)/Hb? Fe(II) is a one‐electron‐transfer reaction process coupled with one‐proton‐transfer. In addition the effect of scan rate on peak currents and peak separation potential was investigated and electrochemical parameters such as α and k_s were calculated. In the second part of this work, the ability of the electrode for determination of Hb concentration was investigated. The results showed a linear dynamic range from 0.15 to 2 µM and a detection limit of 0.11 µM. The relative standard deviation is 4.1 % for 4 successive determinations of a 1 µM Hb solution.     

Synthesis and evaluation of novel arylisoxazoles linked to tacrine moiety: in vitro and in vivo biological activities against Alzheimer’s disease

Molecular Diversity - Alzheimer’s disease (AD) is now ranked as the third leading cause of death after heart disease and cancer. There is no definite cure for AD due to the multi-factorial...