Synthesis and Biological Evaluation of Pyrazoline and Pyrrolidine-2,5-dione Hybrids as Potential Antitumor Agents

In search of novel and effective antitumor agents, pyrazoline-substituted pyrrolidine-2,5-dione hybrids were designed, synthesized and evaluated in silico, in vitro and in vivo for anticancer efficacy. All the compounds exhibited remarkable cytotoxic effects in MCF7 and HT29 cells. The excellent antiproliferative activity toward MCF7 (IC₅₀=0.78±0.01 μM), HT29 (IC₅₀=0.92±0.15 μM) and K562 (IC₅₀=47.25±1.24 μM) cell lines, prompted us to further investigate the antitumor effects of the best compound S2 (1-(2-(3-(4-fluorophenyl)-5-(p-tolyl)-4,5-dihydro-1H-pyrazol-1-yl)-2-oxoethyl)pyrrolidine-2,5-dione). In cell-cycle analysis, S2 was found to disrupt the growth phases with increased cell population in G₁/G₀ phase and decreased cell population in G₂/M phase. The excellent in vitro effects were also supported by inhibition of anti-apoptotic protein Bcl-2. In vivo tumor regression studies of S2 in HT29 xenograft nude mice, exhibited equivalent and promising tumor regression with maximum TGI, 66 % (i. p. route) and 60 % (oral route) at 50 mg kg⁻¹ dose by both the routes, indicating oral bioavailability and antitumor efficacy. These findings advocate that hybridization of pyrazoline and pyrrolidine-2,5-dioes holds promise for the development of more potent and less toxic anticancer agents.     

Application of fly ash on the growth performance and translocation of toxic heavy metals within Cajanus cajan L.: Implication for safe utilization of fly ash for agricultural production

The present study was undertaken to examine the influence of the application of fly ash (FA) into garden soil for Cajanus cajan L. cultivation and on accumulation and translocation of hazardous metals from FA to edible part. Numerous studies have been reported on the growth and yield of agricultural crops under FA stress; however, there is a dearth of studies recommending the safe utilization of fly ash for crop production. Pot experiments were conducted on C. cajan L., a widely cultivating legume in India for its highly nutritious seeds. C. cajan L. were grown in garden soil and amended with varying concentrations of FA in a weight/weight ratio (0%, 25%, 50% and 100%; w/w). Incorporation of fly ash from 25% to 100% in garden soil increases the levels of pH, particle density, porosity and water holding capacity from 3.47% to 26.39%, 3.98% to 26.14%, 37.50% to 147.92% and 163.16% to 318.42%, respectively, than the control while bulk density decrease respectively from 8.94% to 48.89%. Pot experiment found that accumulation and translocation of heavy metals in tested plant depends on the concentration of FA. Addition of FA at lower concentration (25%) had shown positive results in most of the studied parameters of growth and yield (14.23% than control). The experimental results confirmed that lower concentration of FA (25%) is safe for C. cajan cultivation, which not only enhanced the yield of C. cajan L. significantly but also ensured the translocation of heavy metals to edible parts within the critical limits.     

A comparison of rate sensitive constitutive equations under plane stress conditions

Summary Numerical dynamic solutions of the circular hole enlargement problem for a thin plate, due to a constant acceleration imposed at the hole boundary, have been used for comparing different models for describing rate sensitive visco-plastic materials. In the constitutive equations that have been compared, the visco-plastic part of the strain rate is an exponential, linear, cubic and fifth power function of the overstress above the static stress-strain curve. Stress histories and the variation of the plate thickness, at the hole radius, have been computed for different rates of loading, and for a wide range of the parameter describing the visco-plastic behaviour of the material. The relative usefulness of the different models, for a complex state of stress and strain, has been assessed by comparing the numerical solutions for the different models.

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Ein Vergleich geschwindigkeitsabhängiger Werkstoffgleichungen für den ebenen Spannungszustand

Zusammenfassung Es werden numerische Lösungen für das dynamische Problem der Aufweitung eines Kreislochs in einer dünnen Scheibe, wobei eine konstante Beschleunigung am Lochrand vorgeschrieben wird, verwendet, um verschiedene, geschwindigkeitsabhängige viskoplastische Materialmodelle zu vergleichen. In den miteinander verglichenen Materialgesetzen ist der viskoplastische Teil der Verzerrungsgeschwindigkeit eine Funktion, die entweder exponentiell, linear, kubisch oder fünften Grades der Spannungszunahme gegenüber der statischen Spannungs-Dehnungskurve ist. Die Spannungsgeschichte und die Änderung der Plattendicke genommen am Lochumfang werden für verschiedene Belastungsgeschwindigkeiten und für einen weiten Bereich der Parameter des viskoplastischen Materialverhaltens berechnet. Die relative Brauchbarkeit der verschiedenen Modelle für komplizierte Spannungs- und Verformungszustände wird durch einen Vergleich der numerischen Lösungen abgeschätzt.

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With 11 Figures

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Department of Mechanical Engineering, Institute of Technology Banaras Hindu University, Varanasi, India     

Theoretical and experimental studies of the LCC-typeparallel resonant converter

Using the state-plane approach, the steady-state analysis and design of a high-frequency LCC-type parallel resonant converter (LCC PRC) operating in the continuous conduction mode are carried out. On the basis of this analysis, a set of steady-state characteristic curves for the LCC PRC is plotted. Various design curves for component value selection and device ratings are also presented. A simple design procedure is given, and a design example for a 150 W, 140 kHz multioutput LCC PRC power supply is presented for illustrative purposes. A prototype unit has been built and verifies the theoretical results     

Growth kinetics studies of multifilamentary Nb3Sn formed by the bronze process

A systematic study of growth kinetics of Nb₃Sn formation is reported for multifilamentary conductors in the bronze process. At all reaction temperatures studied, the rate controlling step is found to be the diffusion of tin through the grain boundaries of the layer. The growth law R = ktⁿ is obeyed and the measured values of the time exponent n are in accordance with growth kinetics models. The reaction rate constant k shows an optimum behaviour for samples annealed at 725°C. The results indicate that growth kinetics plays a significant role in determining T_C, the superconducting critical temperature of the Nb₃Sn layer.     

Fluid—particle heat transfer in fixed and fluidized beds

Fluid-particle heat transfer in fixed and fluidized beds is re-examined. The heat transfer factor depends not only on the particle Reynolds number but also on the void fraction of the bed. The available experimental data has been correlated to yield a non-linear relationship between ?J_h and the particle Reynolds number. The resulting expression is:

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Magneto-optical effects in temperature-sensitive ferrofluids

A temperature-dependent magneto-optical study of three different temperature-sensitive fluids was carried out. The changes in transmitted intensity as a function of applied magnetic field and temperature are recorded. The study provides an alternative technique for determining the Curie temperature of such fluids, and it is also feasible for the monitoring of temperature changes of such fluids optically within a limited time span.