Computer-Aided Search for 5-Arylideneimidazolone Anticancer Agents Able To Overcome ABCB1-Based Multidrug Resistance

ABCB1 modulation is an interesting strategy in the search for new anticancer agents that can overcome multidrug resistance (MDR). Hence, 17 new 5-arylideneimidazolones containing an amine moiety, as potential ABCB1 inhibitors, were designed, synthesized, and investigated. The series was tested in both parental (PAR) and multidrug-resistant (MDR) ABCB1-overexpressing T-lymphoma cancer cells using cytotoxicity assays. The ABCB1-modulating activity was examined in rhodamine 123 accumulation tests, followed by Pgp-Glo™ Assay to determine the influence of the most active compounds on ATPase activity. Lipophilic properties were assessed both, in silico and experimentally (RP-TLC). Pharmacophore-based molecular modelling toward ABCB1 modulation was performed. The studies allowed the identification of anticancer agents (p-fluorobenzylidene derivatives) more potent than doxorubicin, with highly selective action on MDR T-lymphoma cells (selectivity index >40). Most of the investigated compounds showed ABCB1-modulating action; in particular, two 5-benzyloxybenzylidene derivatives displayed activity nearly as strong as that of tariquidar.     

Investigation of some organic binders

These studies concern residues of the vacuum petroleum distillation of crude oil, used as binders for briquetting comminuted materials. The residues have been separated into the group components asphaltenes, resins, and oils. Chemical analyses of these components and calculations of some structural parameters by means of the Hazelwood and van Krevelen methods have been carried out on all these materials in order to indicate differences between the residues. The chemical constitutions of the binders examined do not differ basically but there are differences between some physical and rheological properties (viscosity, ductility), electrical properties (specific resistance, dielectric loss factor) and in molar refraction and in the carbon aromaticity (from volatile matter).     

Some aspects of the carbonization of vacuum distillation residue from crude oil

These studies concern the carbonization process of residues from vacuum distillation of crude oil. Some explanation aspects of the hypothetic reaction mechanism controlling the carbonization of high molecular weight components of crude oil are developed. On the basis of numerous experimental investigations, the thermal decomposition process can be divided into two stages, the first, from 670 to 790 K, in which the decomposition reactions take place and low and medium weight molecular compounds are emitted and the second stage, from above 790 K to 1000 K, in which cyclization, condensation and aromatization processes take place, and the degree of structural ordering in the solid products increases.     

Grafting of poly(acrylic acid) on polyamide yarn

Graft copolymerization of acrylic acid onto PA6 yarn was examined in this study. Prior to the grafting process, the fibers were activated with a benzene solution of benzoyl peroxide. Next, the fibers were put into a bath containing acrylic acid, a dispersing agent, and the activator of reaction. The effects of the main process parameters and auxiliary additives on the degree of grafting, quantity of the homopolymer formed during grafting, effectiveness of grafting, extent of conversion, and grafting ratio were determined. Using calculation factors such as the reaction efficiency, the extent of reaction, and the ratio of grafting, the conditions of grafting were found that made possible the reduction or elimination of the by‐product. Also determined were the influence of the degree of grafting on the moisture sorption and the swelling of modified fibers. In addition, the value of apparent activation energy was calculated (49.123 kJ/mol). © 2001 John Wiley & Sons, Inc. J Appl Polym Sci 80: 1914–1919, 2001     

Polyurethane/Polylactide-Based Electrospun Nonwovens as Carriers for Human Adipose-Derived Stromal Stem Cells and Chondrogenic Progenitor Cells

Articular cartilage dysfunctions are major cause of pain and disability and lead to serious health complications. Cell-based therapies are proposed as treatment methods for cartilage regeneration. In this study, we proposed polyurethane/poly(L-lactide-co-D, L-lactide)-based electrospun nonwovens as carriers for the delivery of human adipose-derived stromal stem cells. We found that 6:4 and 8:2 polyurethane/poly(L-lactide-co-D, L-lactide) initially enhance proliferative rate of human adipose-derived stromal stem cells, shorten their population doubling time, promote creation of functional chondrogenic nodules during chondrogenic differentiation, improve the collagen-2-to-collagen-1 protein ratio, and upregulate the expression of collagen-2 and aggrecan genes.     

The investigations of gas‐powder two phase flow in packed bed

Gas‐powder two‐phase flow in packed beds was investigated and the results are presented in this paper. The experimental system, in which the glass powder and air gas were injected into the lower part of the packed bed allowed the estimation of the influence of gas velocity, powder feed rate, powder and packed particles diameter on pressure loss and total hold up of powder in the packed bed. On the base of the experimental results, a one‐dimensional mathematical model for gas‐powder two‐phase flow in the packed bed was developed. This model allows satisfactory prediction of the pressure loss and the hold ups of powders. The maximum deviation between calculated and measured values was less than ±15%. Futhermore, the conditions when the blockade of the flow occurs were defined. The additional pressure loss (expressed by F_k) due to the gravitional force of powders and the collision and the friction between powders and packed particles, was correlated with Froude number as: for the void fraction in the packed bed ?₀ of between 0.36 to 0.41 or .     

Magnetic resonance studies of cement based materials in inhomogeneous magnetic fields

Single-sided magnets give hope that Nuclear Magnetic Resonance (NMR) might in future be used for in situ characterisation of hydration and water transport in the surface layers of concrete slabs. Towards that end, a portable NMR-MOUSE (MObile Universal Surface Explorer) has been used to follow the hydration of gypsum based plaster, a Portland cement paste and concrete mortar. The results compare favourably to those obtained using a standard laboratory bench-top spectrometer. Further, stray field imaging (STRAFI) based methods have been used with embedded NMR detector coils to study water transport across a mortar/topping interface. The measured signal amplitudes are found to correlate with varying sample conditions.     

New derivatives of phenylamine as novel building blocks of conducting polymers

A novel phenylamine substituted derivatives possessing different photochromic groups were investigated. Using the electrochemical and spectroelectrochemical measurements the electrochemical activity of the monomers and polymers have been studied. The results indicate good film forming properties most of the monomers and stability of the forming films. The polymeric films include diphenylamine or triphenylamine unit and five member heterocycle ring moieties.