Anthranilamide-pyrazolo[1,5-a]pyrimidine conjugates as p53 activators in cervical cancer cells

A library of new anthranilamide-pyrazolo[1,5-a]pyrimidine conjugates were designed, synthesized, and evaluated for their anticancer activity in cervical cancer cells such as HeLa and SiHa that possess low levels of p53. All 24 conjugates showed antiproliferative activity, while some of them exhibit significant cytotoxicity. In assays related to cell-cycle distribution, these conjugates induced G(2) /M arrest in HeLa cells and G(1) cell-cycle arrest in SiHa cells. Immunocytochemistry assays revealed that these compounds cause nuclear translocation of p53, thereby indicating the activation of p53. In cervical cancer cells, the p53 protein is degraded by E6 oncoprotein. Immunoblot and RT-PCR analyses proved the presence of mitochondria-mediated apoptosis with involvement p53 target genes such as BAX, Bcl2, and p21 (CDKI). Moreover, these compounds increased the phosphorylated forms of p53 and provide signals for apoptosis induction. Interestingly, one of the conjugates, (2-phenyl-7-(3,4,5-trimethoxyphenyl)pyrazolo[1,5-a]pyrimidin-5-yl)(4-(2-(thiophen-2-ylmethylamino)benzoyl)piperazin-1-yl)methanone, is the most promising candidate in this series and has the potential to be taken up for further detailed studies.     

Zirconia Nanoparticles Made in Spray Flames at High Production Rates

Synthesis of zirconia nanoparticles by flame spray pyrolysis (FSP) at high production rates is investigated. Product powder is collected continuously in a baghouse filter unit that is cleaned periodically by air-pressure shocks. Nitrogen adsorption (BET), X-ray diffractometry (XRD), transmission electron microscopy (TEM), and thermogravimetric analysis (TGA) are used to characterize the product powder. The effect of powder production rate (up to 600 g/h), dispersion gas flow rate, and precursor concentration on product particle size, crystallinity, morphology, and purity is investigated. The primary particle size of zirconia is controlled from 6 to 35 nm, while the crystal structure consists of mostly tetragonal phase (80–95 wt%), with the balance monoclinic phase at all process conditions. The tetragonal crystal size is close to the primary particle size, which indicates weak agglomeration of single crystals.     

Viscosity estimation of triacylglycerols and of some vegetable oils, based on their triacylglycerol composition

The experimentally determined kinematic viscosities of simple triacylglycerols [trilaurin, trimyristin (MMM), tripalmitin (PPP), tristearin (SSS), triolein (OOO), and trilinolein (LiLiLi) were correlated to a modified Andrade-type equation. The constants for the modified equation were derived for each simple triacylglycerol. The method was also used to estimate the viscosity of mixed triacylglycerols [1,2-dimyristoyl-3-palmitoyl (MMP), 1,2-dioleoyl-3-palmitoyl (OOP), 1,2-dimyristoyl-3-oleoyl (MMO), and 1,2-dipalmitoyl-3-oleoyl (PPO)], binary triacylglycerol mixtures (PPO/OOP, PPP/SSS, and OOO/SSS of different portions), and three types of vegetable oils [refined, bleached, and deodorized palm oil; cocoa butter; and canola oil] by applying modified Kay’s rule utilizing the simple triacylglycerol constants derived earlier. In all cases, the estimated values for liquid viscosity were compared with experimental values determined in this work and with previous work from the literature. When applied to vegetable oils, the method requires knowledge of their triacylglycerol composition. Despite its simplicity, the method gives a reasonable estimate. The method may be used to predict the viscosity of different blends of vegetable oils, and the accuracy is expected to increase when more experimental data on simple triacylglycerols become available.     

A kinetic study of the hydrolytic degradation of polyethylene terephthalate at high temperatures

The hydrolytic depolymerization of molten PET in excess water was studied using a 2 L stirred pressure reactor at temperatures of 250, 265, and 280°C. Rate constants for hydrolysis are calculated from the initial rate data. At initial water: PET charge ratios (w/w) exceeding 5.1, essentially complete depolymerization to monomer is possible at 265°C. At lower water: PET initial charges, an equilibrium is established. The equilibrium constants are calculated for 2 g water/g PET at three temperatures. A kinetic model is proposed to describe the hydrolysis reaction. The model is shown to fit experimental data and to yield good predictions for the equilibrium concentration of carboxyl groups. Carboxyl-group concentrations are measured using an end-group analysis technique. Potentiometric titrations are carried out in one of two solvent systems, dimethylphenol:chloroform or dimethylsulfoxide, depending on the extent of hydrolysis. © 1993 John Wiley & Sons, Inc.     

Quality Evaluation of Groundwater Resources using Geostatistical Methods (Case Study: Central Lorestan Plain,Iran)

In this research, based on the qualitative data of 40 wells, variations of water quality parameters of the Central Plain Aquifer were evaluated using kriging and IDW (Inverse Distance Weighting) methods. Owing to the normal distribution of the studied parameters (except Na⁺, SO₄^2?, and TH: total hardness), ordinary kriging was used for modeling. The analysis of the data trends indicated that all the variables were influenced by in two general trends, i.e., NW–SE and NE–SW. In fact, these trends were a result of the effect of the structural conditions on aquifer properties such as transmissivity and flow direction. Variogram analysis (based on C₀ near zero and C₀/σ² ratio between 0.0–0.5) showed that the Na⁺, TDS (total dissolved solids), Ca²⁺, and TH variables have a good spatial structure and the BOD (biochemical oxygen demand), COD (chemical oxygen demand), NO₃^?, and EC variables have poor spatial structure. The BOD, COD, NO₃^?, and EC (electrical conductivity) variables have the smallest range and isotropic distribution. On the other hand, the Ca²⁺, Mg²⁺, Na⁺, SO₄^2?, Cl^?, HCO₃^?, pH, TDS, TH and Alk (alkalinity) parameters are characterized by anisotropic distributions. The Na⁺, TDS, Ca²⁺, and TH variables have the largest range. The results showed that both the IDW and kriging methods have close estimates to one another. The pH variable decreases toward the outlet whereas the EC and TDS variables increase along the direction of water flow and toward the outlet. The distributions of the BOD and COD variables do not perfectly match with the aggregation of industrial activities in the central part as well as the agricultural activities in the southeastern and central parts of the aquifer. The distributions of the Ca²⁺, Mg²⁺, and Alk variables completely follow the geology condition and regional spread of carbonate formations. The Na⁺ concentration increases from the center toward the outlet. The concentration of the Cl^? variable is the highest in the central part of the plain due to the concentration of agricultural and industrial activities. The distribution of the SO₄^2? variable is influenced by a natural factor (lithology), especially in the southeastern parts and the outlet as well as artificial factors (agricultural and industrial activities) in the central and southeastern parts of the aquifer. The NO₃^? variable, which is directly influenced by agricultural and livestock-farming activities, has its maximum concentration in the southeastern areas.