Synthesis, computational study and biological evaluation of 9-acridinyl and 1-coumarinyl-1,2,3-triazole-4-yl derivatives as topoisomerase II inhibitors

Topoisomerase (IIB) inhibitors have been involved in the therapies of tumour progression and have become a major focus for the development of anticancer agents. New three-component hybridised ligands, 1,4-disubstituted-1,2,3-triazoles (8–17), were synthesised via a 1,3-dipolar cycloaddition reaction of 9-azidoacridine/3-azidocoumarin with N/O-propargyl small molecules under click reaction conditions. Cancer cell growth inhibition of the synthesised triazoles was tested against human cell-lines in the NCI-60-cell-panel, and the most active compounds tested against topoisomerase (IIB)-enzymes. The acridinyl ligands (8–10) revealed 60–97% cell growth inhibition in six cancer cell-panels. Cell-cycle analysis of MCF7 and DU-145 cells treated with the active acridinyl ligands exhibited cell-cycle arrest at G2/M phase and proapoptotic activity. In addition, compound 8 displayed greater inhibitory activity against topoisomerase (IIB) (IC50 0.52 µM) compared with doxorubicin (IC50 0.83 µM). Molecular dynamics simulation studies showed the acridine–triazole–pyrimidine hybrid pharmacophore was optimal with respect to protein–ligand interaction and fit within the binding site, with optimal orientation to allow for intercalation with the DNA bases (DG13, DC14, and DT9)

Hydrothermal Preparation of Gd+3 -Doped Titanate Nanotubes: Magnetic Properties and Photovoltaic Performance

Pure and Gd+3 -doped titanate nanotubes (TNTs) materials were synthesized by a hydrothermal method. Their morphology, optical properties, thermal stability, and magnetic properties were characterized by X-ray diffraction (XRD), transmission electron microscope (TEM), UV-Vis spectroscopy, thermal analysis, and magnetic measurements. It was found that doping renders Gd+3-TNT visible light active and results in smaller crystallite size and larger surface area as well as higher thermal stability compared to pure titanate nanotubes. The estimated magnetic moments point to presence of weak antiferromagnetic interaction. Application of the prepared Gd+3-TNT for modifying conventional photoanodes in polymer solar cells was attempted. Preliminary results show slightly improved photovoltaic energy conversion efficiency in the devices containing the newly designed Gd+3 -doped nanotubes

Hepatitis B virus (HBV) genotypes in Egyptian pediatric cancer patients with acute and chronic active HBV infection

<p>Abstract</p> <p>Background</p> <p>There are eight genotypes of hepatitis B virus (A-H) and subgenotypes are recognized. Genotyping can be accomplished based on a partial sequence of HBV genome such as the pre-S or S gene. Several methods have been developed and used for HBV genotyping. This study was undertaken to determine the HBV genotypes in Egyptian pediatric cancer patients with acute and chronic liver disease.</p> <p>Methods</p> <p>HBV genotypes were determined in 22 patients who had acute forms of liver disease (AH) and in 48 patients with chronic active hepatitis (CAH). A type-specific primer based the nested-PCR method was employed in the HBV genotyping.</p> <p>Results</p> <p>This study showed that HBV infections in pediatric cancer patients are attributed predominantly to viral genotypes D and B that constituted 37.1% and 25.7%, respectively of the total infections. In addition, there was a relatively high prevalence of mixed infections of 15.7% among the studied group especially mixed A/D genotype infections. Genotype D was found significantly more often in patients with CAH than in patients with AH [23/48(47.9%) <it>v </it>3/22 (13.6%)].</p> <p>Conclusion</p> <p>These findings show the distribution of HBV A-D genotypes in pediatric cancer Egyptian patients. Furthermore, our results indicate a markedly high prevalence of mixed A/D genotype infections in subjects with CAH and a possible association of mixed infections with the severity of liver diseases.</p

Crystal and Molecular Structure of Acylalmino Derivatives of 1-(2,4,6-Trichlorophenyl)-4,5-dihydropyrazol-5-one

The structure of acylamino derivatives of 1-(2,4,6-trichlorophenyl)-4,5- dihydropyrazol-5-one was studied by X-ray diffraction. 3-Acetylamino-1- (2,4,6-trichlorophenyl)-4,5-dihydropyrazol-5-one and 3-benz-oylamino-1-(2,4,6- trichlorophenyl)-4,5-dihydropyrazol-5-one exist in crystal as CH tautomers. The nature and number of acylamino groups were found to affect the nature of intermolecular hydrogen bonds in the crystals studied

Investigation of Er3+ Ions Reinforced Zinc-Phosphate Glasses for Ionizing Radiation Shielding Applications

Melt quenching technique is used for preparing glasses with chemical formula (70P2 O5)– (16 − x)CdO–(14ZnO)–(xEr2 O3), (x = 1–6 mol%). These glasses were named Er1, Er2, Er3, Er4, Er5, and Er6, respectively. Photon buildup factors, fast neutron absorption, and electron stopping of the prepared glasses were examined. Glasses’ density was varied from 3.390 ± 0.003 for the Er1 glass sample to 3.412 ± 0.003 for the Er6 glass sample. The Buildup factor (BUF) spectra have relatively higher values in the Compton Scattering (CS) dominated areas compared to both Photoelectric effect (PE), and Pair Production (PP) dominated energy regions. The highest BUF appeared at the Er atom K-absorption edge, whose intensity increases as the molar concentration of Er2 O3 in the glasses increases. The photon absorption efficiency (PAE) of the glasses increases according to the trend (PAE)Er1 &lt; (PAE)Er2 &lt; (PAE)Er3 &lt; (PAE)Er4 &lt; (PAE)Er5 &lt; (PAE)Er6. Fast neutron removal cross-section, FNRC (ΣR) values of the glasses obtained via calculation varied from 0.1045–0.1039 cm−1 for Er1–Er6. Furthermore, the continuous slowing down approximation mode (CSDA) range enhances the kinetic energy of electrons for all glasses. Generally, results revealed that the investigated glasses could be applied for radiation shielding and dosimetric media. © 2021 by the authors. Licensee MDPI, Basel, Switzerland.Taif University Researchers Supporting Project number (TURSP-2020/23), Taif University, Taif Saudi Arabia. "The APC was covered by "Dunarea de Jos" University of Galati, Romania, through grant no. RF3621/2021

Subsystem purity as an enforcer of entanglement

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Incidence of post-harvest disease and airborne fungal spores in a vegetable market

The sampling of bioaerosols has been carried out using a Rotorod sampler as well as by exposing culture plates. The screening of some common vegetables was also done for the isolation of fungi as market pathogens to study post-harvest diseases. Altogether, fifty nine fungal spore types and 78 species of 33 genera belonging to different groups were recorded respectively on the rotorod strips and on exposed Petri dishes. Many saprophytic and pathogenic fungi were found to be associated with sampled vegetables from the market. In all forty-six fungal species belonging to 26 genera were recovered from five varieties of vegetables collected from the same market. The most dominant forms of fungi were of Aspergillus followed by Cladosporium, Penicillium, Alternaria, Fusarium, Curvularia, Trichoderma, and Rhizopus. Aspergillus niger, A. flavus, A. fumigatus, Penicillium spp. and Cladosporium herbarum, found to be dominant during the period of investigation. Important mycotoxin-producing fungi such as A. flavus, A. fumigatus and Fusarium moniliforme were isolated from the vegetables collected from the market