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Herein, a new series of 2-chloro-N-(5-(2-oxoindolin-3-yl)-4H-pyrazol-3-yl) acetamide derivatives containing 1,3,4-thiadiazole (10a - i) and 4H-1,2,4-triazol-4-amine (11a - r) moiety was designed, synthesised as novel anticancer agents. The antiproliferative activity values indicated that compound 10 b stood as the most potent derivative with IC 50 values of 12.0 nM and 10 nM against A549 and K562 cells, respectively. Mechanism investigation and docking studies of 10 b indicated that it possessed good apoptosis characteristic and dose-dependent growth arrest of A549 and K562 cells, blocked cell cycle into G2/M phase. Interestingly, 10 b suppressed the growth of A549 and K562 cells via modulation of EGFR and p53-MDM2 mediated pathway.

The reasons, prevention, and control of loess disaster are of great concern in practice. In recent years, Xi’an city, China, has taken the leadership in large-scale construction of subway lines in the loess strata. To study the structural response of the tunnel in loess region under local hydrodynamic environment, an experimental testing in 1g as well as a numerical simulation were performed, in which the achieved results were verified and were found to be in good agreement. Furthermore, the results showed that when the water outlet point is above the lining, the overall stress of the lining is “peanut shell,” as the water pressure of the outlet point decreases, the tensile stress of the top and bottom of the lining increases, while the compressive stress on both sides decreases; the channel form of the flow to the lining changes with the variation of the position of the water outlet point. It is worth mentioning that in the process of water gushing, the closer to the water source, the greater surface subsidence is, and there is a positive correlation between water pressure and surface subsidence. This study is of significant benchmark for the construction, maintenance, and prevention of tunnel in loess strata under the influence of water environment.

To accelerate face-gear engineering application, a precision grinding method for complex surface of aero face-gear is provided in this paper. Based on the principle of face-gear drive, the principle of face-gear grinding by disc wheel is analyzed, and the tooth surface equation of the face-gear is calculated with coordinate transformations. Taking the grinding needs into account, a special machine tool is developed, and movements control method of face-gear grinding by the disc wheel on the machine tool is proposed. To ensure the correct tooth profile of the disc wheel, the method of wheel dressing is provided and the optimum design methods of CNC cutter sites and step sizes selection are provided. To verify the feasibility of the grinding method for face-gear, the simulation of face-gear grinding by disc wheel is performed based on VERICUT software according to the grinding method. The experiments of face-gear grinding and the wheel dressing are carried out finally, and the results show that it is feasible for face-gear grinding using the involute disc wheel and the special machine tool.

While understanding the drivers of river water quality is crucial, the dependence on ground observations hinders the accurate quantification of driver thresholds, as well as the scale-dependent effects of buffer zones. By transcending the limitations of ground observations, satellite remote sensing provides the spatially continuous data required to define effective buffer zones and determine the threshold intervals for natural and anthropogenic drivers, effectively promoting sustainable watershed management. Herein, we determined the total nitrogen (TN), total phosphorus (TP), permanganate index (CODMn), and turbidity in the Minjiang River of Fujian Province by synergizing Sentinel-2 imagery and in situ data (2021–2024). Subsequently, we further employed generalized additive models (GAMs) considering scale-dependent (50 m to 20 km) characteristics to screen and evaluate the natural–anthropogenic factors influencing the water quality indicators. The GAMs revealed that TN exhibited multiphasic responses to forest cover and water area, characterized by alternating positive and negative effects across their range. TP was found to be predominantly driven by agricultural and urban land use, showing clear scale–threshold effects. This study provides an integrated framework that moves beyond retrieval to quantitatively assess the impact of multi-scale natural–anthropogenic factors, offering actionable insights for precise watershed zoning and science-based management for the sustainable development of river systems.

Bearing is the core component of high‐speed rotating machinery. However, the lubricating oil plays an important role in reducing the temperature and the collision between components. It can improve the performance of the bearing under high‐speed rotation. Therefore, based on the theory of oil‐air two‐phase flow, this paper establishes a numerical analysis flow‐heat model of ball bearing under different oil supply. At the same time, the vibration is calculated. The influence of internal oil‐air field and thermal characteristics on vibration is analyzed. The results show that the volume of oil is not uniformly distributed in the bearing chamber. The oil gradually decreases from the outer ring to the inner ring. It is mainly concentrated on the oil‐air inlet. With the increasing of oil supply speed, the temperature of the bearing decreases firstly and then increases, and there is an optimal oil supply speed. The inner ring vibration velocity is basically similar to the temperature trend. Meanwhile, the lowest temperature is mainly concentrated near the oil‐air inlet. The maximum error between simulation results and experimental results is 11.37%. Finally, the reliability of the simulation analysis is verified by the temperature and vibration experiment. It provides some theoretical support for the optimization of oil‐air lubrication parameters of angular contact ball bearings.

In this paper, first, the meso-debonding process of a GAP/CL20/AP composite solid propellant under uniaxial tension was analyzed using the advantages of the material point method (MPM) and the finite element method (FEM) for the first time; then, the numerical simulation results were compared with the experiments. Based on the basic principle of modeling with the material point method, grains of different sizes were generated quickly and efficiently. Next, the grains were dispersed into particles, and the position information of the particles was mapped onto the background grid, so the background grids were used to determine the position of the grains. After that, the generated AP and CL20 grains were imported into the commercial software Abaqus through python scripting codes for numerical calculation. Based on macro-mechanical tests and a micro-numerical simulation, this paper studies the micro-internal mechanism that affects the macro-mechanical properties of composite solid propellants. Three interface parameters needed to be determined by parameter inversion, and the value of the objective interpolation function minR was 0.05078%. From a comparison, it was found that the numerical simulation results are in good agreement with the experimental results in the aspects of micro-crack cracking characteristics and the nominal stress–strain curve of propellants. After that, the influence of interface parameters on the stress–strain curve are discussed. The research in this paper has high scientific value and engineering application value and can provide important reference and guidance for the design of composite solid propellants and its mechanical property analyses, so as to solve the structural integrity problem of solid rocket motor charges.

Replacing natural aggregate (NA) with recycled aggregate (RA) has contributed to the trend of sustainable development in civil construction. With this background, improvements in the mechanical properties of recycled aggregate concrete (RAC) and the scientific design of the mixture ratio are attracting more concern in recent years. This paper is a review of the recent research, including the following aspects: the mixture design of RAC; the improved mechanical properties of recycled concrete with steel fibers; and the performance of the main components. In addition, the primary composition materials, properties, and calculation methods of the mixture ratio of RAC are summarized. The mechanical properties, durability and microscopic analysis of RAC are also discussed. The accurate calculation of mixture proportion can significantly facilitate the work of preparing a test mix of RAC. Through the mixture-ratio optimization and physical and chemical strengthening of RA, the mechanical properties of RAC can be improved to promote the wider application of this eco-friendly material.

Xiao-Ban-Xia-Tang (XBXT), a traditional Chinese medicine formula, has been used for the treatment of emesis for nearly 2000 years, but its underlying mechanism is not yet fully clarified. The purpose of this study is to reveal the antiemetic mechanisms of XBXT by focusing on the NLRP3 inflammasome pathway in a chemotherapy-induced rat pica model. The pica model was generated by a single intraperitoneal injection of cisplatin in this study. Consumption of kaolin (a type of clay) and food and body weight were recorded every 24 hours. Cisplatin-induced increase in kaolin consumption (pica) was used to quantify chemotherapy-induced nausea and vomiting (CINV). Tissue from the ileum and antrum was stained with hematoxylin eosin (HE) to observe pathological changes. The levels of reactive oxygen species (ROS) and inflammatory cytokines, including IL-1β and IL-18 in serum, were detected by ELISA. In addition, changes in the NLRP3 inflammasome activation in the ileum and antrum were investigated using western blot and immunofluorescence microscopy. The results showed that oral administration of XBXT and ondansetron inhibited acute and delayed pica and significantly protected against the gastrointestinal pathological injury induced by cisplatin. The levels of ROS, IL-1β, and IL-18 in the serum of cisplatin-treated rats were also remarkably decreased by XBXT and ondansetron. Moreover, we found that XBXT can inhibit cisplatin-induced NLRP3 inflammasome activation. The present study indicates that the inhibition of the NLRP3 inflammasome activation might be one of the potential mechanisms for the therapeutic effects of XBXT against CINV.

As a group of diversified frameworks, quinazolin derivatives displayed a broad field of biological functions, especially as anticancer. To investigate the quantitative structure-activity relationship, 3D-QSAR models were generated with 24 quinazolin scaffold molecules. The experimental and predicted pIC50 values for both training and test set compounds showed good correlation, which proved the robustness and reliability of the generated QSAR models. The most effective CoMFA and CoMSIA were obtained with correlation coefficient r 2 ncv of 1.00 (both) and leave-one-out coefficient q 2 of 0.61 and 0.59, respectively. The predictive abilities of CoMFA and CoMSIA were quite good with the predictive correlation coefficients ( r 2 pred ) of 0.97 and 0.91. In addition, the statistic results of CoMFA and CoMSIA were used to design new quinazolin molecules.

Through the years, the seismic resistance of underground structures has attracted more and more attention, and dynamic characteristics of metro station is one of the most important issues. In this article, the 3D numerical model of Zhang Wangqu metro station along Metro Line 5 in Xi'an is established to study on seismic dynamic response of roof, floor, columns and beams in the island platform metro station. Compared with the earthquake damage of Dakai metro station in the Kobe M7.2 Earthquake and the shaking table test of metro station in loess area, results reveal that horizontal acceleration can reflect seismic wave characteristics under the horizontal seismic wave; the maximum relative displacement of roof and floor, the maximum axle force and shear force at transfer node are bigger than the standard section and reduce with the increase of buried depth; the maximum axle force and shear force of columns increases from top to bottom. The island platform metro station should focus on the structural settings of transfer node, and the columns and beams here must select materials with greater strength.