Synthesis of a new family of acyclic nucleoside phosphonates, analogues of TPases transition states

A 6-step procedure was developed for the synthesis of a new family of acyclic nucleoside phosphonates (ANPs), "PHEEPA" [(2-pyrimidinyl-2-(2-hydroxyethoxy)ethyl)phosphonic acids] in overall yields ranging from 4.5% to 32%. These compounds, which possess on one side a hydroxy function and on the other side a phosphonate group, can be considered either as potential antiviral agents or as transition state analogues of nucleoside phosphorylases such as thymidine phosphorylase.     

A Mild and Highly Efficient Method for the Preparation of Silyl Ethers using Fe(HSO4)3/Et3N by Chlorosilanes

A very efficient and mild procedure for preparation of silyl ethers from benzylic, allylic, propargilic alcohols, phenols, naphtoles and some of phenolic drugs with trimethylsilylchloride (TMSCl), triethylsilylchloride (TESCl) and t‐buthyldimethylsilyl chloride (TDSCl) ethers in the presence of Fe(HSO₄)₃/Et₃N in room temperature in excellent yields is reported. This procedure also allows the excellent selectivity for silylation of alcohols and phenols.     

Cyclopalladated complexes of 2-phenylaniline and their catalytic activity in Suzuki and Heck reactions under mild conditions

A series of palladium complexes bearing monodentate and bidentate ligands were applied in the Suzuki reaction of aryl halides and the Heck reaction of styrene with phenylboronic acid. The complexes were found to be effective catalysts for these reactions affording the cross-coupled products in moderate to excellent yields.     

Antimicrobial agents as photostabilizers for rigid poly(vinyl chloride)

Some amide derivatives of ethylene glycol‐bis(2‐aminoethylether)‐N,N,N^′,N^′‐tetraacetic acid (EGTA) have been prepared via their coupling with different aniline derivatives: amino, methyl, chloro, and hydroxy aniline. The EGTA amide derivatives were characterized, and their antimicrobial activities were evaluated. These antimicrobial agents have been investigated as photostabilizers for rigid poly(vinyl chloride) (PVC), suspension PVC, with a K value of 70. Their stabilizing efficiencies were evaluated by determining the percentage of weight loss, the intrinsic viscosities, as well as the amount of formed gel of the photodegraded PVC. The extent of discoloration and the change in the mechanical properties of the photodegraded polymer were also evaluated. The applied materials reduced the loss in weight that resulted from HCl evolution during photodegradation. Both viscosity and gel content measurements showed also a decrease in their values during the degradation process. The decrease in the percentage of gel formation upon applying the investigated photostabilizers reflects the lowering in extent of cross‐linking of the polymer, which implies preserving the mechanical properties of PVC. The extent of discoloration was also improved in the presence of the investigated compounds. The results have proved a greater stabilizing efficiencies of the antimicrobial EGTA amide derivatives than that of the phenyl salicylate ultraviolet (UV) absorber, which is commonly used as an industrial stabilizer. A radical mechanism was proposed to account for the stabilizing action of the investigated products. Copyright © 2011 John Wiley & Sons, Ltd.     

Fabrication of Chitosan‐Multiwall Carbon Nanotube Nanocomposite Containing Ferri/Ferrocyanide: Application for Simultaneous Detection of D‐Penicillamine and Tryptophan

We report a simple and effective strategy for fabrication of the nanocomposite containing chitosan (CS) and multiwall carbon nanotube (MWNT) coated on a glassy carbon electrode (GCE). The characterization of the modified electrode (CS‐MWNT/GC) was carried out using scanning electron microscopy (SEM) and UV–vis absorption spectroscopy. The electrochemical behavior of CS‐MWNT/GC electrode was investigated and compared with the electrochemical behavior of chitosan modified GC (CS/GC), multiwalled carbon nanotube modified GC (MWNT/GC) and unmodified GC using cyclic voltammetry (CV) and electron impedance spectroscopy (EIS). The chitosan films are electrochemically inactive; similar background charging currents are observed at bare GC. The chitosan films are permeable to anionic Fe(CN)₆^3?/4? (FC) redox couple. Electrochemical parameters, including apparent diffusion coefficient for the Fe(CN)₆^3?/4? redox probe at FC/CS‐MWNT/GC electrode is comparable to values reported for cast chitosan films. This modified electrode also showed electrocatalytic effect for the simultaneous determination of D‐penicillamine (D‐PA) and tryptophan (Trp). The detection limit of 0.9 μM and 4.0 μM for D‐PA and Trp, respectively, makes this nanocomposite very suitable for determination of them with good sensitivity.     

Expression of miRNAs Targeting <Emphasis Type="Italic">mTOR</Emphasis> and <Emphasis Type="Italic">S6K1</Emphasis> Genes of mTOR Signaling Pathway Including miR-96, miR-557, and miR-3182 in Triple-Negative Breast Cancer

Triple-negative breast cancer (TNBC) is a highly aggressive form of breast cancer. Aberrant expression of genes in mTOR pathway and their targeting miRNAs plays an important role in TNBC. The aim of this study was to determine the expression of mTOR and S6K1 and their targeting miRNAs in breast cancer cell lines and clinical samples. miRNAs targeting 3′-UTR of mTOR and S6K1 mRNAs were predicted using bioinformatic algorithms. MDA-MB-231, MCF-7, and MCF-10A as well as 20 TNBC samples were analyzed for gene and miRNA expression using quantitative real-time PCR (RT-qPCR). A receiver operating characteristic (ROC) curve analysis was performed for evaluation of candidate miRNAs as diagnostic biomarkers. miR-96 and miR-557 targeting mTOR and S6K1 mRNAs, respectively, were selected, and miR-3182 was selected as the miRNA targeting both genes. The miRNAs were down-regulated in cell lines, while their target mRNAs were up-regulated. Similar findings were observed in clinical samples. The ROC curve analysis revealed decline in expression of these miRNAs. We suggest that miR-96, miR-557, and miR-3182 can be used as inhibitory agents for mTOR and S6K1 in TNBC-targeted therapy.     

Enhanced properties of photovoltaic devices tailored with novel supramolecular structures based on reduced graphene oxide nanosheets grafted/functionalized with thiophenic materials

For verifying the influence of donor–acceptor supramolecules on photovoltaic properties, different hybrids were designed and used in organic solar cells. In this respect, reduced graphene oxide (rGO) was functionalization with 2‐thiophene acetic acid (rGO‐f‐TAA) and grafted with poly(3‐dodecylthiophene) (rGO‐g‐PDDT) and poly(3‐thiophene ethanol) (rGO‐g‐PTEt) to manipulate orientation of poly(3‐hexylthiophene) (P3HT) assemblies. Face‐on, edge‐on, and flat‐on orientations were detected for assembled P3HTs on rGO and its functionalized and grafted derivatives, respectively. Alteration of P3HT orientation from face‐on to flat‐on enhanced current density (J _sc), fill factor (FF), and power conversion efficiency (PCE) and thus J _sc = 7.11 mA cm^?2, FF = 47%, and PCE = 2.14% were acquired. By adding phenyl‐C71‐butyric acid methyl ester (PC71BM) to active layers composed of pre‐designed P3HT/rGO, P3HT/rGO‐f‐TAA, P3HT/rGO‐g‐PDDT, and P3HT/rGO‐g‐PTEt hybrids, photovoltaic characteristics further improved, demonstrating that supramolecules appropriately mediated in P3HT:PC71BM solar cells. Phase separation was more intensified in best‐performing photovoltaic systems. Larger P3HT crystals assembled onto grafted rGOs (95–143 nm) may have acted as convenient templates for the larger and more intensified phase separation in P3HT:PCBM films. The best performances were reached for P3HT:P3HT/rGO‐g‐PDDT:PCBM (J _sc = 9.45 mA cm^?2, FF = 54%, and PCE = 3.16%) and P3HT:P3HT/rGO‐g‐PTEt:PCBM (J _sc = 9.32 mA cm^?2, FF = 53%, and PCE = 3.11%) photovoltaic systems. © 2017 Wiley Periodicals, Inc. J. Polym. Sci., Part B: Polym. Phys. 2017 , 55 , 1877–1889