Synthesis and Anti-Cancer Activity of New Pyrazolinyl-Indole Derivatives: Pharmacophoric Interactions and Docking Studies for Identifying New EGFR Inhibitors

Newly designed series of indole-containing pyrazole analogs, pyrazolinylindoles, were synthesized, and their structures were confirmed based on the spectral data of the ¹H NMR, ¹³C NMR, and HR-MS analyses. Preliminary anti-cancer activity testings were carried out by the National Cancer Institute, United States of America (NCI, USA). Compounds HD02, HD05, and HD12 demonstrated remarkable cytotoxic activities against nine categories of cancer types based cell line panels which included leukemia, colon, breast, melanoma, lungs, renal, prostate, CNS, and ovarian cancer cell lines. The highest cytotoxic effects were exhibited by the compounds HD02 [1-(5-(1-H-indol-3-yl)-3-(p-tolyl)-4,5-dihydro-1H-pyrazol-1-yl)-2-phenylethanone], HD05 [1-(3-(4-chlorophenyl)-5-(1H-indol-3-yl)-4,5-dihydro-1H-pyrazol-1-yl)-2-phenoxyethanone], and HD12 [(3-(4-chlorophenyl)-5-(1H-indol-3-yl)-4,5-dihydro-1H-pyrazol-1-yl)(pyridin-4-yl)methanone] against some of the 56 types of NCI-based cell lines in different panels. Compound HD05 showed the maximum range of cancer cell growth inhibitions against all categories of the cell lines in all nine panels. On average, in comparison to the referral standard, imatinib, at a dose level of 10 µM, the HD05 showed significant activity against leukemia in the range of 78.76%, as compared to the imatinib at 9% of cancer cells’ growth inhibitions. Molecular docking simulation studies were performed in silico on the epidermal growth factor receptor (EGFR) tyrosine kinase, in order to validate the activity.     

Prediction of axial velocity profiles and solids hold-up in a rotary kiln

Axial bed depth profiles were experimentally measured in a rotary kiln containing ilmenite particles under steady state and transient conditions. The variables include feed rate of solids, inclination and rotational speed of the kiln. and dam height. The variation of the axial velocity with kiln axis was estimated. The semi-experimental model proposed by Perron and Bui (1990) was modified to include the effect of the variables of the present study. The mean residence time of solids was estimated from the fractional hold-up and expressed in terms of the process variables. The transients induced by a step change in any of the operating conditions were measured as variation of discharge rate of solids with time.     

A Novel Highly Sensitive Humidity Sensor Based on ZnO/SBA‐15 Hybrid Nanocomposite

This work deals with the study of hydrothermally synthesized zinc oxide (ZnO) loaded mesoporous SBA‐15 hybrid nanocomposite for relative humidity sensing (RH) at room temperature. The sensor exhibits an excellent ~5 orders impedance change along with excellent linearity, quick response time (17 s), rapid recovery time (18 s), negligible hysteresis (1.2%), good repeatability, and stability (1.8%) in 11%–98% RH range. In addition, complex impedance spectra of the sensor at different RHs were analyzed to understand the humidity sensing mechanism. Our study can open a new way for realizing ZnO/SBA‐15 hybrid nanocomposite for fabrication of high‐performance RH sensors.     

Revisiting the size selective performance of EPA's high-volume total suspended particulate matter (Hi-Vol TSP) sampler

Under the National Ambient Air Quality Standard (NAAQS) for airborne lead, measurements are conducted by means of a high-volume total suspended particulate matter (Hi-Vol TSP) sampler. In the decade between 1973 and 1983, there were 12 publications that explored the sampling characteristics and effectiveness of the Hi-Vol TSP, yet there persists uncertainty regarding its performance. This article presents an overview of the existing literature on the performance of the Hi-Vol TSP, and identifies the reported sampler effectiveness with respect to four factors: particle size (reported effectiveness of 7%–100%), wind speed (?36% to 100%), sampler orientation (7%–100%), and operational state (107%–140%). Effectiveness of the Hi-Vol TSP was evaluated with a solid, polydisperse aerosol in a controlled wind tunnel setting. Isokinetic samplers were deployed alongside the Hi-Vol TSP to investigate three wind speeds (2, 8, and 24 km h^?1), three sampler orientations (0°, 45°, 90°), and two operational states (on, off) for aerosols with aerodynamic diameters from 5 to 35 µm. Results indicate that particle diameter was the largest determining factor of effectiveness followed by wind speed. Orientation of the sampler did not have a significant effect at 2 and 8 km h^?1 but did at 24 km h^?1. In a passive state, the Hi-Vol TSP was collected between 1% and 7% of available aerosol depending on particle size and wind speed. Results of this research do not invalidate results of previous studies but rather contribute to our overall understanding of the Hi-Vol TSP's size-selective performance. While results generally agreed with previous studies, the Hi-Vol TSP was found to exhibit less dependence on these four factors than previously reported.

© 2017 American Association for Aerosol Research     

Structural characteriztion of Nd-doped in silica host matrix prepared by net chemical process

Silica host matrix containing neodymium which is potentially important for the formation of nanocrystalline metal oxides was prepared by solgel method, using tetra-ethoxysilane and Nd(NO3)3 as precursor materials. The prepared samples were changed from amorphous to nanocrystallites phase at sintered temperature 550℃ (4 h), 750℃ (8 h) and 950 ℃ (12 h). The thermally treated sample microstructures were investigated using X-ray diffraction (XRD), Fourier transformation infrared spectroscopy (FTIR), and scanning electron microscopy (SEM). While a further increase of the temperature at 750 ℃ and annealing time (8 h) resulted in the formation of cubic and hexagonal Nd2O3 nanocrystallites. At constant sintering temperature 950℃ for 12 h, the samples showed sharper and intense peaks. The sizes of Nd2O3 nanocrystallites were characterized by XRD with average size～46 nm.     

Optimization of fermentation condition for co-production of ethanol and 2,3-butanediol (2,3-BD) from hemicellolosic hydrolysates by Klebsiella oxytoca XF7

Microbial production of ethanol and 2,3-butanediol (2,3-BD) from agro-residues has been attracting interest because of their applications in various industries, including generation of biofuel molecules. In the present investigation, the hemicellulosic fraction of corncob was hydrolyzed by indigenous holocellulase from novel psychrotolerant Aspergillus niger SH3 resulting in high xylose release (34.61?g?L^?1), followed by the bioconversion of xylose to ethanol and 2,3-BD. Taguchi design was adopted to optimize the process which resulted in 5.25- and 3.31-fold increase in 2,3-BD (12.18?±?0.53?g?L^?1) and ethanol (4.08?±?0.03?g?L^?1), as compared with un-optimized condition. For the first time, co-production of ethanol and 2,3-BD from the corncob hemicellulosic hydrolysate was performed using a newly isolated Klebsiella oxytoca XF7 strain, under the optimized fermentation conditions. These results suggest that K. oxytoca XF7 is a promising candidate for co-production of ethanol and 2,3-BD, with high xylose conversion efficiency (96.65%), facilitating the economical production of biofuel molecules.     

Saponin-loaded SBA-15: release properties and cytotoxicity to Panc-I cancer cells

In this study, first time a nanoformulation, saponin-loaded SBA-15 has been developed for an improved and continuous release. The SBA-15 nanopowder was synthesized by a hydrothermal process. Saponin was introduced into the mesoporous channels of SBA-15 and its concentration in SBA-15 was measured by UV–visible spectrophotometry. The pristine SBA-15 and saponin-loaded SBA-15 were characterized by small-angle XRD, FESEM, HRTEM, TGA, FTIR. N₂ adsorption–desorption isotherms were used to measure the specific surface area and pore channel structure parameters of pristine and loaded SBA-15. Saponin release was studied in phosphate buffered saline (pH 7.4), which revealed that the release rate could be effectively controlled. The controlled drug release is highly desired for cancer treatment. The cytotoxicity of pristine and loaded SBA-15 was analyzed on Panc-I cancer cells. Both the pristine SBA-15 and saponin-loaded SBA-15 nanoparticles showed specific toxicity on the cancer cells. The preliminary results showed that saponin-loaded SBA-15 could be an effective therapeutic agent for Panc-I cancer cells.     

Anthocyanin-rich fruit vinegar from Grewia and Cantaloupe fruit blends

Grewia is a tropical berry rich in anthocyanins and antioxidants but highly perishable in nature. In this study, desirable composite blend of overripe Grewia (Phalsa) berries and cantaloupe was sought for conversion to acetic acid. Composition of raw macerate, and the alcoholic and acetic ferments was analysed for sugars, alcohol and acetic acid. The primary alcohol yield varied significantly (5.75–99.44%) with blend composition. Vinegar from select blend attained 4.98% acidity with 138.57 mg mL⁻¹ of phenols and high anthocyanins retention (74.77%). Gompertz model was used to fit the growth curves of S. cerevisiae and A. aceti (R²> 0.92) during fermentation. Presence of ethyl acetate, iso-pentyl alcohols explained pleasant sweet fruity aroma of resulting vinegar. Thus, high quality functional red fruit vinegar can be obtained to prevent spoilage and utilise the functional potential of this delicate and nutritious berry.     

Optimal dynamic emergency reserve activation using spinning,hydro and demand-side reserves

This paper proposes an optimal dynamic reserve activation plan after the occurrence of an emergency situation (generator/transmission line outage, load increase or both). An optimal plan is developed to handle the emergency, using the coordinated action of fast and slow reserves, for secure operation with minimum overall cost. It considers the reserves supplied by the conventional thermal generators (spinning reserves), hydro power units and load demands (demand-side reserves). The optimal backing down of costly/fast reserves and bringing up of slow reserves in each sub-interval in an integrated manner is proposed. The proposed reserve activation approaches are solved using the genetic algorithm, and some of the simulation results are also compared using the Matlab optimization toolbox and the general algebraic modeling system (GAMS) software. The simulation studies are performed on the IEEE 30, 57 and 300 bus test systems. These results demonstrate the advantage of the proposed integrated/dynamic reserve activation plan over the conventional/sequential approach.     

Performance analysis of diamond search algorithm over full search algorithm

Microsystem Technologies - Motion estimation is a progression used to estimate motion vectors between two or more images with a high degree of temporal redundancy. It is commonly used in video...