Development of Potent Adenosine Monophosphate Activated Protein Kinase (AMPK) Activators

Previously, we reported the identification of a thiazolidinedione‐based adenosine monophosphate activated protein kinase (AMPK) activator, compound 1 (N‐[4‐({3‐[(1‐methylcyclohexyl)methyl]‐2,4‐dioxothiazolidin‐5‐ylidene}methyl)phenyl]‐4‐nitro‐3‐(trifluoromethyl)benzenesulfonamide), which provided a proof of concept to delineate the intricate role of AMPK in regulating oncogenic signaling pathways associated with cell proliferation and epithelial–mesenchymal transition (EMT) in cancer cells. In this study, we used 1 as a scaffold to conduct lead optimization, which generated a series of derivatives. Analysis of the antiproliferative and AMPK‐activating activities of individual derivatives revealed a distinct structure–activity relationship and identified 59 (N‐(3‐nitrophenyl)‐N′‐{4‐[(3‐{[3,5‐bis(trifluoromethyl)phenyl]methyl}‐2,4‐dioxothiazolidin‐5‐ylidene)methyl]phenyl}urea) as the optimal agent. Relative to 1 , compound 59 exhibits multifold higher potency in upregulating AMPK phosphorylation in various cell lines irrespective of their liver kinase B1 (LKB1) functional status, accompanied by parallel changes in the phosphorylation/expression levels of p70S6K, Akt, Foxo3a, and EMT‐associated markers. Consistent with its predicted activity against tumors with activated Akt status, orally administered 59 was efficacious in suppressing the growth of phosphatase and tensin homologue (PTEN)‐null PC‐3 xenograft tumors in nude mice. Together, these findings suggest that 59 has clinical value in therapeutic strategies for PTEN‐negative cancer and warrants continued investigation in this regard.     

The preparation of flat H–Si(111) surfaces in 40% NH4F revisited

The reasons why ideally flat H–Si(111) surface can be prepared by NH₄F etching are investigated from correlation between AFM observations and experimental conditions used for etching. It is shown that pitting may be completely suppressed if a one side polished wafer is immersed in an oxygen free solution. An analytical electrochemical study of the (111) and rough face of the same n-Si wafer is presented to yield insight into observations.     

Clicking ferrocene to halogenated boron-doped diamond surfaces

The halogenated boron-doped diamond (BDD) surfaces were reacted with sodium azide through a nucleophilic substitution reaction. The resulting azide-terminated BDD surfaces were used to trigger the "click" reaction. Because of the attractive electrochemical properties of ferrocene-containing molecules, such as fast electron transfer rates, reversible redox activities, and favorable redox potentials, we show that ferrocene derivatives can be grafted onto non-oxidized diamond surfaces by click"chemistry". These redox-active ferrocene-containing layers on a BDD surface, because of their ability to store and release charges reversibly, have the potential to be used as hybrid molecular/semiconductor memory devices.     

Design of 2-D Linear Phase Digital Filters Using Schur Decomposition and Symmetries

In this paper we present a new and numerically efficient technique for designing 2-D linear phase octagonally symmetric digital filters using Schur decomposition method (SDM) and the diagonal symmetry of the 2-D impulse response specifications. This technique is based on two steps. First, the 2-D impulse response matrix is decomposed into a parallel realization of k sections, each comprising two cascaded linear phase SISO 1-D FIR digital filters. It is shown that using the symmetry property of the 2-D impulse response matrix and the fact that the left and right eigenspaces obtained by SDM are transpose of each other, the design problem of two 1-D digital filters is reduced to the design problem of only one 1-D digital filter in each section.     

Multi-impregnating pitch-bonded Egyptian dolomite refractory brick for application in ladle furnaces

A method of preparation of multi-impregnated pitch-bonded Egyptian dolomite refractory brick for ladle furnace is described. Brick samples were prepared from blend of calcined dolomite mineral and coal tar pitch. The blend was hot mixed and pressed under a compression force up to 151 MPa. Green bricks were baked for 2 h at temperatures up to 1000 °C. Voids in the baked bodies were filled with carbon by multiple impregnations using low-softening point coal tar pitch. Each impregnation step (30 min) was followed by calcination at 1000 °C. Brick samples containing 8–12 wt.% coal tar pitch binder and pressed under 108–151 MPa acquired quantify crushing strength. However, multi-impregnating favored the mechanical strength of the baked brick samples and improved their hydration resistance (>45 days). Dolomite brick samples containing 10 wt.% coal tar pitch and pressed at 108 MPa gave high hydration resistance (more than 60 days in normal condition) compared to the hydration resistance of the commercial bricks (30 days). The prepared brick samples have acceptable density, chemical stability, outstanding resistance and good mechanical properties would meet the requirements of Ladle furnace (LF) for steel making industry. In addition, estimation of production cost of the brick indicates it is competitive with the market price based on durability and service life time aspects.     

Degradation of Polycarbonate Properties Under Thermal Aging

Journal of Failure Analysis and Prevention - The aim of this paper is to characterize the thermal aging effect near the glass transition temperature of polycarbonate (PC) at different hold time....     

Automatic source scanner identification using 1D convolutional neural network

In this digital world, digitized documents can be considered original or a piece of evidence; checking the authenticity of any suspicious image has become an unavoidable concern to preserve the trust in its legitimacy. However, identifying the source of a digital image without any prior embedded information is a very challenging task. This paper proposes a novel one-dimensional convolutional neural network (1D-CNN) model to solve the source scanner identification (SSI) problem blindly. Unlike traditional methods based on handcrafted features, the proposed framework can dynamically learn and extract scanner device-specific features. This work, comprised of the 1D-CNN and a support vector machine (SVM) as a classifier, was trained on nine scanners of different brands and models. The experimental result shows that our model achieves 98.15% accuracy on full images and overall accuracy of 93.13% on segments from test images, outperforming other state-of-art approaches. Our model also proves to be able to distinguish between scanners of the same model. Furthermore, the SVM classifier improved the 1D-CNN accuracy by approximately 3% compared to its original configuration.

     

Structural Stabilities and Elastic Thermodynamic Properties of SrTe Compound and SrTe<Subscript>1−<Emphasis Type="Italic">x</Emphasis></Subscript>Ca<Subscript><Emphasis Type="Italic">x</Emphasis></Subscript> Alloy Under High Pressure

The effect of pressure on the structural, elastic, and thermodynamic properties of SrTe in both B1 (rocksalt) and B2 (CsCl-type) phases and the SrTe_1?x Ca _x alloys with Ca dopant concentrations at x = 0.16667, 0.20, 0.33333, 0.42857, 0.44444 and 0.50 have been investigated using the two new gradient-corrected functional developed by Perdew, J.P.; Burke, K.; Ernzerhof named Density-Gradient Expansion for Exchange in Solids (PBEsol) and generalized Wu–Cohen (WC), in a significant range of pressure from 0 GPa to 30 GPa. The structure parameters, elastic stiffness constants c _ij , the bulk modulus (B), Kleinman parameter (\( \xi \)), shear anisotropies A _shear are also determined. Furthermore, as reported in this study, the aggregate elastic modulus (B, G, E), Poisson’s ratio (ν) and the Lame’s coefficients (λ) are estimated. On the other hand, the ductility, brittleness, longitudinal, transverse sound velocities and the Debye temperature Θ_D(T) are also obtained. Importantly, our results are in reasonable agreement with the available theoretical and experimental data. To the best of our knowledge, this is the first study of the effect of the composition on the properties of the SrTe_1?x Ca _x alloys which may encourage other works for the confirmation of the reported results.     

First-principle calculations of elastic and electronic properties of the filled skutterudite CeFe4P12

A theoretical study of elastic and electronic properties of the filled skutterudite CeFe₄P₁₂ is presented, using the full-potential linear muffin–tin orbital (FP-LMTO) method. In this approach the local spin density approximation (LSDA) was used for the exchange-correlation (XC) potential. Results are given for lattice constant, bulk modulus, its pressure derivative and elastic constants. Our calculations performed for band structure and density of state show that this compound is an indirect band gap material (Γ–N). The results are compared with previous calculations and experimental data.     

Development and validation of a coupled heat and mass transfer model for green roofs

This paper describes a dynamic model of transient heat and mass transfer across a green roof component. The thermal behavior of the green roof layers is modeled and coupled to the water balance in the substrate that is determined accounting for evapotranspiration. The water balance variations over time directly impact the physical properties of the substrate and the evapotranspiration intensity. This thermal and hydric model incorporates wind speed effects within the foliage through a new calculation of the resistance to heat and mass transfer within the leaf canopy. The developed model is validated with experimental data from a one-tenth-scale green roof located at the University of La Rochelle. A comparison between the numerical and the experimental results demonstrates the accuracy of the model for predicting the substrate temperature and water content variations. The heat and mass transfer mechanisms through green roofs are analyzed and explained using the modeled energy balances, and parametric studies of green roof behavior are presented. A surface temperature difference of up to 25 °C was found among green roofs with a dry growing medium or a saturated growing medium. Furthermore, the thermal inertia effects, which are usually simplified or neglected, are taken into account and shown to affect the temperature and flux results. This study highlights the importance of a coupled evapotranspiration process model for the accurate assessment of the passive cooling effect of green roofs.