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72.
The natural xanthone α-mangostin (αM) exhibits a wide range of pharmacological activities, including antineoplastic and anti-nematode properties, but low water solubility and poor selectivity of the drug prevent its potential clinical use. Therefore, the targeted third-generation poly(amidoamine) dendrimer (PAMAM G3) delivery system was proposed, based on hyperbranched polymer showing good solubility, high biocompatibility and low immunogenicity. A multifunctional nanocarrier was prepared by attaching αM to the surface amine groups of dendrimer via amide bond in the ratio 5 (G32B12gh5M) or 17 (G32B10gh17M) residues per one dendrimer molecule. Twelve or ten remaining amine groups were modified by conjugation with D-glucoheptono-1,4-lactone (gh) to block the amine groups, and two biotin (B) residues as targeting moieties. The biological activity of the obtained conjugates was studied in vitro on glioma U-118 MG and squamous cell carcinoma SCC-15 cancer cells compared to normal fibroblasts (BJ), and in vivo on a model organism Caenorhabditis elegans. Dendrimer vehicle G32B12gh at concentrations up to 20 µM showed no anti-proliferative effect against tested cell lines, with a feeble cytotoxicity of the highest concentration seen only with SCC-15 cells. The attachment of αM to the vehicle significantly increased cytotoxic effect of the drug, even by 4- and 25-fold for G32B12gh5M and G32B10gh17M, respectively. A stronger inhibition of cells viability and influence on other metabolic parameters (proliferation, adhesion, ATP level and Caspase-3/7 activity) was observed for G32B10gh17M than for G32B12gh5M. Both bioconjugates were internalized efficiently into the cells. Similarly, the attachment of αM to the dendrimer vehicle increased its toxicity for C. elegans. Thus, the proposed α-mangostin delivery system allowed the drug to be more effective in the dendrimer-bound as compared to free state against both cultured the cancer cells and model organism, suggesting that this treatment is promising for anticancer as well as anti-nematode chemotherapy.  相似文献   
73.
This paper presents an analysis of mechanical damage carried out on ‘Golden Delicious’ apple variety, which was subjected to impact loads during free drop against various rigid plates. For this purpose, an analysis of the contact pressure based on determined contours and surface pressure distributions at the contact point between the fruit dropped from various heights against fixed hard plates was performed. The impact test was conducted by means of Tekscan® system supported by computer verifying analysis. To obtain impact loads as well as their courses, the surface pressures and the bruise volumes were determined. Furthermore, use of ultra-thin pressure sensors allowed for determination of the characteristic shape of contact area and the impact of fruit onto rigid plate. The results showed that the impact of fruit against rigid surface (concrete, wood) generates high values of maximum surface pressure and the bruise volume, observed at dropping from 10 mm. A decrease in hardness of the test material (polyethylene foam) with decreasing maximum surface pressure approximately twice was noticed. The polyethylene foam is one of the best materials which protect fruit from mechanical damage, confirmed by the relation of bruise surface to contact surface, which did not exceed 35% during the impact at 150 mm. The results of proposed studies can contribute to developing of harvest, handling, and transport processes, aiming at reduction in losses among fruit growers and production costs, i.e., by improvement of transport method.  相似文献   
74.
Cyclodextrins (CDs) are highly respected for their ability to form inclusion complexes via host–guest noncovalent interactions and, thus, ensofance other molecular properties. Various molecular modeling methods have found their applications in the analysis of those complexes. However, as showed in this review, molecular dynamics (MD) simulations could provide the information unobtainable by any other means. It is therefore not surprising that published works on MD simulations used in this field have rapidly increased since the early 2010s. This review provides an overview of the successful applications of MD simulations in the studies on CD complexes. Information that is crucial for MD simulations, such as application of force fields, the length of the simulation, or solvent treatment method, are thoroughly discussed. Therefore, this work can serve as a guide to properly set up such calculations and analyze their results.  相似文献   
75.
Corrosion of the metal oxide surface of cupronickel (CuNi) alloys is a problem in applications such as household water pipes, industrial pipelines, and marine vessels. On other substrates, thin films have been used as barriers to corrosion. Here, the formation of self-assembled monolayers (SAMs) on the CuNi metal oxide surface has been investigated. Stable, well-ordered SAMs of octadecylphosphonic acid (ODPA) and 16-phosphonohexadecanoic acid (COOH-PA) were formed on the metal oxide surface of CuNi foils (55% Cu/45% Ni) using a solution deposition method. The ODPA modified surfaces could be used to provide a non-reactive barrier that inhibits corrosion of the CuNi metal oxide surface. Meanwhile, COOH-PA films could be used for further surface reactions such as surface initiated polymerization, in which polymer coatings are grown directly from a well-ordered film. Film-modified surfaces were characterized using diffuse reflectance infrared Fourier transform spectroscopy, contact angle analysis, and matrix assisted laser desorption ionization time of flight mass spectrometry. The ability of the films to inhibit corrosion by limiting oxidation of the CuNi surface was assessed using cyclic voltammetry.  相似文献   
76.
The electrical properties of deep-level defects in real packaged SiC Schottky barrier rectifiers were studied by deep level transient spectroscopy (DLTS). One deep-level trap with an activation energy in the 0.29–0.30 eV range was revealed to be present in all the tested samples. The electrical characteristics of the trap indicate it is probably attributed to dislocations or to metastable defects, which can be responsible for discrepancies observed in I-V characteristics (see Ref. [2]).  相似文献   
77.
The technological problems occurring in the co-firing of biomass and brown coal (lignite) prompted this research project. During the fuel preparation, accidental self-ignition and explosions were several times reported by power plants operators. The aim of this study was to evaluate brown coal, sunflower husks and sunflower husk pellets as fuels for co-firing in energetic boilers. Sunflower husk had a lower ash content and calorific value than the pellets. The range of the combustion temperatures of the biomass (200–300 °C) was narrower than that of brown coal (200–800 °C). The formation of highly alkaline ash from the biomass resulted in the formation in boiler of agglomerates of ash. The elemental composition, thermogravimetric and biological analyses suggested that the pellets contained synthetic additives difficult to identify. The biological method was proposed for evaluating biomass additives. The use of additional agents in the pelletizing process may influence on the combustion parameters. Mixing biomass with brown coal may occasionally result in self-ignition in the logistic chain. Plastic additives and biological activity may contribute to self-ignition.  相似文献   
78.
The effects of thermo-mechanical treatment on selected properties related to the structure of Fe-0.85Mo-0.65i-1.4C powder metallurgy (PM) steel are reported. Three kinds of initial microstructure of specimens, i.e., pearlite + ferrite + cementite, martensite + retained austenite and α + spheroidized cementite were examined. Processing was carried out on a plastometer-dilatometer Bähr machine by compression cylindrical specimens at 775 °C at a strain rate of 0.001 s?1. X-ray diffraction was carried out with symmetrical Bragg-Brentano and grazing incident angle methods on a D8-Advance diffractometer with filtered radiation of cobalt CoK α . The following features were determined: texture, density of dislocations, density of vacancies, lattice parameter of Fe α and mean size of crystallites. Significant differences in structure were observed, especially in quenched specimen, as a result of the thermo-mechanical treatment. Regardless of initial state of the specimens, the determined properties were on a similar level. Crystallite size was in the range 97-106 nm, crystallite texture (I{200}/I{110}) × 10 = 1.15-1.62 and density of vacancies I{110}/I{220} = 7.06-7.52.  相似文献   
79.
The paper presents an attempt to develop a probabilistic model for predicting an annual number of storm overflow discharges. Forecasting the occurrence of an overflow discharge event involved the application of the logistic regression, which does not require the development of complex hydrodynamic catchment models. The performed calculations showed that the logistic regression model can be successfully used to evaluate the performance of the emergency overflow weir. The resultant logit model eliminates the necessity to develop hydrodynamic models, to conduct continuous measurements of the flow intensity in the stormwater drainage system and to collect detailed information on the characteristics of the subcatchments within the analyzed catchment. The hydrodynamic model was used to simulate the annual number of discharges. The analysis of the results demonstrated that they are in the range of stochastic values, which indicates an application-related character of the method.  相似文献   
80.
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