Aurora kinase B (AKB) is a crucial signaling kinase with an important role in cell division. Therefore, inhibition of AKB is an attractive approach to the treatment of cancer. In the present work, extensive quantitative structure–activity relationships (QSAR) analysis has been performed using a set of 561 structurally diverse aurora kinase B inhibitors. The Organization for Economic Cooperation and Development (OECD) guidelines were used to develop a QSAR model that has high statistical performance (R2tr = 0.815, Q2LMO = 0.808, R2ex = 0.814, CCCex = 0.899). The seven-variable-based newly developed QSAR model has an excellent balance of external predictive ability (Predictive QSAR) and mechanistic interpretation (Mechanistic QSAR). The QSAR analysis successfully identifies not only the visible pharmacophoric features but also the hidden features. The analysis indicates that the lipophilic and polar groups—especially the H-bond capable groups—must be present at a specific distance from each other. Moreover, the ring nitrogen and ring carbon atoms play important roles in determining the inhibitory activity for AKB. The analysis effectively captures reported as well as unreported pharmacophoric features. The results of the present analysis are also supported by the reported crystal structures of inhibitors bound to AKB. 相似文献
We perceive big data with massive datasets of complex and variegated structures in the modern era. Such attributes formulate hindrances while analyzing and storing the data to generate apt aftermaths. Privacy and security are the colossal perturb in the domain space of extensive data analysis. In this paper, our foremost priority is the computing technologies that focus on big data, IoT (Internet of Things), Cloud Computing, Blockchain, and fog computing. Among these, Cloud Computing follows the role of providing on-demand services to their customers by optimizing the cost factor. AWS, Azure, Google Cloud are the major cloud providers today. Fog computing offers new insights into the extension of cloud computing systems by procuring services to the edges of the network. In collaboration with multiple technologies, the Internet of Things takes this into effect, which solves the labyrinth of dealing with advanced services considering its significance in varied application domains. The Blockchain is a dataset that entertains many applications ranging from the fields of crypto-currency to smart contracts. The prospect of this research paper is to present the critical analysis and review it under the umbrella of existing extensive data systems. In this paper, we attend to critics' reviews and address the existing threats to the security of extensive data systems. Moreover, we scrutinize the security attacks on computing systems based upon Cloud, Blockchain, IoT, and fog. This paper lucidly illustrates the different threat behaviour and their impacts on complementary computational technologies. The authors have mooted a precise analysis of cloud-based technologies and discussed their defense mechanism and the security issues of mobile healthcare.
Seeds ofPisum arvense L.w. Weitor were grown in nitrogen-free nutrient solution for one week and then in the same medium but at a different potassium concentrations (0.0, 0.1 and 10mM) for one month. At the end of the experiment the plants were dried and analysed for total nitrogen, organic carbon, and nutrients (Ca, Mg, Na, K, and P). The number of nodules were counted, and their spatial distribution was studied. The nutrient solution was changed twice a week and analysed for total exuded nitrogen.No positive correlation was found between the total number of nodules and the total nitrogen fixed although nitrogen fixed per one hundred nodules was higher in potassiumrich than in potassium-limited conditions.Plants accumulated higher magnesium concentrations in potassium-limited than in potassium-rich conditions. Roots were relatively more rich in nitrogen (dry weight basis) in potassium-rich conditions. At low supply of potassium a significant amount of the nitrogen fixed was exuded.Increasing the potassium supply increased the total dry weight and total nitrogen fixed by plants but decreased the efficiency of energy (nitrogen fixed per dry weight of green leaves) and potassium utilization for both dry weight production and nitrogen fixation (potassium accumulated per dry weight produced or nitrogen fixed). 相似文献
The detection of and recovery from transient faults that cause errors in microprogrammed control units are addressed. Error detection is based upon a particular form of signature analysis, namely the run-time computation of a value (the signature) that depends strictly on the microprogram path (the sequence) under execution. The microprogram is statistically segmented (sequences are defined in a fixed way, at design time), and an anticipated signature is associated with each sequence. At run time, at the start of each sequence the computation of the signature is restarted, whereas at the end the computed signature is compared with the anticipated signature of the sequence. If the check is passed, the status of the control unit is saved in suitable registers, and the previously saved status is discarded. If the check fails, the last-saved status is restored (rolled back) and microprogram execution restarts from this last-saved point 相似文献
The solid flow inside a blast furnace is modelled using a standalone finite element program and a constitutive equation called hypo‐plastic, in order to better simulate the granular material behaviour. The parameters of this constitutive equation are calibrated using data obtained from simple soil mechanics tests on coke and sinter materials, such as triaxial and oedometric devices. Steady velocity, stress and void fraction fields are obtained after several iterations of the code. Knowledge of the solids velocity field makes it possible to determine the dead man profile, as well as its renewal kinetics. Burden trajectories and time lines are also computed. Knowledge of the stress field makes it possible to compute pressures acting on the burden as well as on the walls. Finally, knowledge of void fraction field makes it possible to determine gas paths. The solid flow model was validated on 2D and 3D small‐scale cold blast furnaces, but the simulations never required any tuning parameter. This code is in fact an invaluable tool to determine the effect of blast furnace profile on solid flow conditions, and reciprocally. 相似文献
In the paper, the performance of HFC125 as an alternative to CFC502 and R22 is assessed under different operating conditions. Cycle characteristics, such as the thermal capacity, coefficient of performance, pressure ratio, system pressures, temperatures, and compressor power are also discussed. Results obtained after extensive detailed experimental work indicate that the performance is degraded on using HFC125, relative to that obtained with HCFC22. 相似文献
We have investigated the possibility that large rock salt formations might be suitable as target masses for detection of neutrinos of energies about 10 PeV and above. In neutrino interactions at these energies, the secondary electromagnetic cascade produces a coherent radio pulse well above ambient thermal noise via the Askaryan effect. We describe measurements of radio-frequency attenuation lengths and ambient thermal noise in two salt formations. Measurements in the Waste Isolation Pilot Plant, located in an evaporite salt bed in Carlsbad, NM yielded short attenuation lengths, 3–7 m over 150–300 MHz. However, measurements at United Salt's Hockley mine, located in a salt dome near Houston, Texas yielded attenuation lengths in excess of 250 m at similar frequencies. We have also analyzed early ground-penetrating radar data at Hockley mine and have found additional evidence for attenuation lengths in excess of several hundred meters at 440 MHz. We conclude that salt domes, which may individually contain several hundred cubic kilometer water-equivalent mass, provide attractive sites for next-generation high-energy neutrino detectors. 相似文献
Summary This paper describes a preliminary set of results concerning novel systems in which the synthesis of furanic polyesters was conducted according to a transesterification procedure. Regular linear macromolecular structures were thus obtained with molecular weights well above those previously reported for similar polyesters prepared by more conventional routes. 相似文献
A rapid instrumental method and protocol is described for the photometric assay of the appearance of cytologic objects in hematology. The study of the effect of stain dilution on the appearance of cells is used to illustrate the efficacy of the method. 相似文献
A formula containing Compactrol, Ac-Di-Sol, Aerosil 200 and talc was used to prepare directly-compressed tablets of indomethacin and its sodium and meglumine salts. The prepared tablets were evaluated for uniformity of weight and thickness, hardness, friability and content uniformity. Each batch was then divided into two, one was coated with an opaque non-enteric film coat and evaluated for coat thickness uniformity. The dissolution rates of the uncoated and coated tablets and the effect of shelf-storage, at room temperature for 11 months, on drug contents were also studied. Indomethacin meglumine tablets showed the least relative standard deviation of weight and thickness. They exhibited acceptable uniformity of content and coat thickness, and the highest hardness-friability ratio. Also exhibited, uncoated and coated, the best in-vitro release of its drug contents and the maximal stability. 相似文献