On the correlation between order parameter, superconducting volume fraction and critical current density in R: 123 superconductors

Resistivity and low field ac susceptibility measurements are made on R: 123 superconducting samples with different rare earth elements R. The order parameter dimensionality OPD is deduced from resistivity versus temperature plot using the Aslamazov and Larkin expression, while the analysis of the temperature dependence of ac susceptibility is done employing Beans’ critical state model and with the help of the Ravi expression. With increasing R, the critical temperatures T_c are nearly kept constant (∼90 K), while the crossover temperatures T_o are shifted to lower values. Moreover, the superconducting order parameter OPD is shifted toward 2D behavior. On the other hand, the values of superconducting volume fraction f_g decrease with increasing ac field amplitude H_m for all samples and it is higher in Er: 123 sample than in Nd: 123 sample. Although the values of critical current density J_c at the peak temperature T_m are nearly unchanged with increasing R, the values of J_c(T), at T<T_m and T>T_m, are found to be dependent on the chosen R. The correlation between the above calculated parameters against R is also mentioned.     

6-Amino-2-thio- and 6-Aminouracils as Precursors for the Synthesis of Antiviral and Antimicrobial Methylenebis(2-thiouracils), Tricyclic Pyrimidines,and 6-Alkylthiopurine-2-ones

Summary. Several derivatives of 5-arylmethylenebis(1-methyl-6-amino-2-thiouracils) and 5-aryldipyrimidopyridines were prepared by stirring of 6-amino-1-methyl-2-thiouracil and 6-amino-1-benzyluracil with different aromatic aldehydes in ethanol in the presence of HCl or refluxing with AcOH. On the other hand, 6-alkylthio-3,9-dimethylpurine-2-ones were synthesized by the alkylation of 3,9-dimethyl-6-thioxanthine which was prepared by treatment of 3,9-dimethylxanthine with P₂S₅. The structures of the novel compounds were characterized by spectroscopic methods. The effects of the novel compounds on both HAV and HSV type 1 were investigated. Also, some compounds showed inhibitory effects on Gram-positive and Gram-negative bacteria as well as yeast and fungi. On leave from Chemistry Department, Faculty of Science, Zagazig University, Zagazig, Egypt     

Design and Synthesis of (2-oxo-1,2-Dihydroquinolin-4-yl)-1,2,3-triazole Derivatives via Click Reaction: Potential Apoptotic Antiproliferative Agents

A mild and versatile method based on Cu-catalyzed [2+3] cycloaddition (Huisgen-Meldal-Sharpless reaction) was developed to tether 3,3’-((4-(prop-2-yn-1-yloxy)phenyl)methylene)bis(4-hydroxyquinolin-2(1H)-ones) with 4-azido-2-quinolones in good yields. This methodology allowed attaching three quinolone molecules via a triazole linker with the proposed mechanism. The products are interesting precursors for their anti-proliferative activity. Compound 8g was the most active one, achieving IC₅₀ = 1.2 ± 0.2 µM and 1.4 ± 0.2 µM against MCF-7 and Panc-1 cell lines, respectively. Moreover, cell cycle analysis of cells MCF-7 treated with 8g showed cell cycle arrest at the G2/M phase (supported by Caspase-3,8,9, Cytochrome C, BAX, and Bcl-2 studies). Additionally, significant pro-apoptotic activity is indicated by annexin V-FITC staining.     

Electrical and magnetic properties of coordinated polymers of poly(ethylene glycol) allenyl methyl ether with iron chloride

The coordinated polymer of poly(ethylene glycol) alleneyl methyl ether (PEGA) with iron (III) chloride (PEGA-FeCl₃) was prepared by radical mechanism and characterized by infrared spectroscopy and elemental analyses. The electrical properties were studied using D.C. electrical conductivity. The relationship between the activation energy (ΔE) and the temperature are given to illustrate the behaviour of the polymer. Investigation of the A.C. magnetic susceptibility of the PEGA-FeCl₃ reveals that the sample obeys the Curie–Weiss law to about 100°C, and behaves in a metallic fashion at higher temperatures. A correlation between the conductivity and the magnetic susceptibility of the doped polymer is discussed.     

Synthesis and Antitumor Evaluation of Novel Alkylated Hydantoin and Thiohydantoin Derivatives

Russian Journal of General Chemistry - New alkylated hydantoin as well as 2-thiohydantoins were synthesized for broadening the library of compounds screened for antitumor activity. Antitumor...     

Solvatochromic,acid–base features and time effect of some azo dyes derived from 1,3-benzothiazol-2-ylacetonitrile: Experimental and semiempirical investigations

The solvatochromism and other spectroscopic properties of seven azo dyes were studied, with a particular respect to the role of the solvent basicity, and interpreted with the aid of experimental findings and semiempirical data. The electronic absorption spectra of the dyes examined in different solvents combined with theoretical calculations showed that most of the investigated compounds coexist in the hydrazone and/or azo-enamine-common anion equilibrium or in the solely anionic form depending upon the nature of the solvent employed. These interesting features open up possibilities for the use of these compounds in analytical chemistry as acid–base indicators. Furthermore, both of intermolecular and intramolecular charge transfer equilibria have been reflected by experimental absorption spectra of compounds 4 and 5. The enthalpies of formation predicted at PM6 (COSMO) and PM6/CI (COSMO) for the ground (S₀) and excited (S₁) states, respectively have been successfully used for the explanation of the observed bathchromic shift in non-polar solvents. The effect of time on the longer wavelength visible band of compound 7 has been thoroughly investigated.     

Stereospecificity of Diels–Alder Reactions Validated Using Ab Initio Calculations: Synthesis of Novel Coumarin and Phenanthridine Derivatives

A new series of coumarin derivatives (2–5) was synthesized by reaction of phenylsulfonylacetonitrile (1) with 2-hydroxy-1-naphthaldehyde and/or salicyaldehyde. Compounds 3 and 5 were converted to the corresponding phenanthridine analogs 6 and 7, respectively. Compound 9a was treated with different dienophiles to furnish the endo adducts of compounds (11a–d) rather than the exo adducts. Ab initio calculations at the Hartree-Fock (HF) level using the basis set 6-31 G (d,p) was used to study and validate the stereospecificity of compounds 11a–d and showed clearly that the endo adducts were thermodynamically favorable. PM3 parameters also showed that the endo adducts are thermodynamically and kinetically favorable. Tetrahydrobenzochromenone (11) was synthesized and allowed to react with different aromatic diazonium salts to give the corresponding 4-arylazo derivatives (13), which were converted to the corresponding diazaindenophenanthrene derivatives (14) by reaction with o-diamines.     

Globally Approved EGFR Inhibitors: Insights into Their Syntheses,Target Kinases,Biological Activities,Receptor Interactions,and Metabolism

Targeting the EGFR with small-molecule inhibitors is a confirmed valid strategy in cancer therapy. Since the FDA approval of the first EGFR-TKI, erlotinib, great efforts have been devoted to the discovery of new potent inhibitors. Until now, fourteen EGFR small-molecule inhibitors have been globally approved for the treatment of different types of cancers. Although these drugs showed high efficacy in cancer therapy, EGFR mutations have emerged as a big challenge for these drugs. In this review, we focus on the EGFR small-molecule inhibitors that have been approved for clinical uses in cancer therapy. These drugs are classified based on their chemical structures, target kinases, and pharmacological uses. The synthetic routes of these drugs are also discussed. The crystal structures of these drugs with their target kinases are also summarized and their bonding modes and interactions are visualized. Based on their binding interactions with the EGFR, these drugs are also classified into reversible and irreversible inhibitors. The cytotoxicity of these drugs against different types of cancer cell lines is also summarized. In addition, the proposed metabolic pathways and metabolites of the fourteen drugs are discussed, with a primary focus on the active and reactive metabolites. Taken together, this review highlights the syntheses, target kinases, crystal structures, binding interactions, cytotoxicity, and metabolism of the fourteen globally approved EGFR inhibitors. These data should greatly help in the design of new EGFR inhibitors.