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961.
Multidrug resistance (MDR), which leads tumors resistance to traditional anticancer drugs, can cause the failure of chemotherapy treatments. Herein, we present a new way to overcome this problem using smart multifunctional graphene‐based drug delivery systems which can target subcellular organelles and show synergistic hyperthermia and chemotherapy. Mitochondria‐targeting ligands are conjugated onto the doxorubicin‐loaded, polyglycerol‐covered nanographene sheets to actively accumulate them inside the mitochondria after charge‐mediated cellular internalization. Upon near‐infrared (NIR) irradiation, adenosine triphosphate (ATP) synthesis and mitochondrial function were inhibited and doxorubicin released into the cellular interior. The hyperthermia‐accelerated drug release led to a highly selective anticancer efficiency, confirmed by in vitro and in vivo experiments.  相似文献   
962.
Nanofibrous polyaniline–magnetite (PANI/Fe3O4) nanocomposite was in situ prepared through adsorption of magnetite nanoparticles onto PANI nanofibers surface and utilized as an efficient sorbent for magnetic solid-phase extraction of naproxen from water and biological samples, followed a desorption step and spectrofluorimetric determination. Field-emission scanning electron microscopy, transmission electron microscopy, Fourier-transform infrared spectroscopy, thermal gravimetric analysis and X-ray diffraction techniques were employed for characterization of the prepared nanocomposite. The important parameters influencing the extraction efficiency including PANI/Fe3O4 mass ratio, adsorbent dose, extraction time, sample solution pH, ionic strength, type and volume of desorption solvent and the elution time were studied and optimized. The investigated nanocomposite was successfully applied to the extraction of naproxen in spiked tap water, urine and plasma samples, with a relative recovery in the range of 90–98%. The reusability of PANI/Fe3O4 was examined for ten successive cycles, and the results confirm that the efficiency did not change significantly. A linear calibration plot was obtained in the range of 40–1000 ng mL?1 with a limit of detection about 17 ng mL?1 under the optimum conditions. The relative standard deviation (RSD) was found to be 2.34% (n = 8, concentration level of 100 ng mL?1). The kinetics and thermodynamics of the extraction process were also studied.  相似文献   
963.
Albumin which is the most abundant drug carrier protein in plasma controls the distribution aspect of drug pharmacokinetics. The aim of this study has been to elucidate the concurrent binding behavior of indomethacin/ibuprofen/heme to HSA under the effect of aspirin-mediated protein acetylation and also to explore the esterase-like catalytic property of the unmodified/modified proteins, as binary or ternary systems, by using various spectroscopic and molecular docking techniques. We found that aspirin-based modification of HSA affects the protein conformation as well as ligand binding at sites I–III. Decrease in pNPA-mediated esterase activity of HSA in different reversible inhibition modes, upon the protein–ligand interactions, was also documented, an issue that may receive considerable attention for computational prodrug design in near future.  相似文献   
964.
G-quadruplexes are formed by association of DNA strands containing multiple contiguous guanines. The capability of drugs to induce formation or stabilize G-quadruplexes is an active area of cancer therapy investigation. We evaluated interaction between two cationic tetrapyridinoporphyrazines with Na+ and K+ forms of human telomeric G-quadruplex DNA by chemometrics method. An antiparallel quadruplex structure was found to be stabilized more greatly by these two isomers in the presence of K+ and Na+ ions. Equilibrium model of a ligand binding with DNA oligomer has been considered as a process of small molecule adsorption on to a lattice of multiple binding sites. In multivariate analysis methods, it is accounted this assertion that during saturation of the macromolecule by a ligand should expect effect of cooperativity due to changes in DNA conformation or the mutual influence between bound ligands. Such phenomenon cannot be entirely described by the classical stepwise complex formation model. From the results of absorption and circular dichroism measurements, the unique site for the ligand binding is suggested to be the intercalating in guanine tetrad plane quadruplex. We found a 2:1 binding stoichiometry for both ligands and Tel22.  相似文献   
965.
In this article, continuing the work done in the previous paper (Fathi et al. in Int. J. Theor. Phys. 51:1938–1945, 2012), we apply a Lagrangian formalism to demonstrate the shape of the geodesic motions for a massive charged particle which is falling freely in a de Sitter spacetime. We will show that a spiral shape of the trajectory is available, due to the logarithmic behavior of time, with respect to the proper time.  相似文献   
966.
In this paper, a simple, convenient and sensitive electrochemical method has been developed for the determination of C.I. Direct Red 80. A gold nanoparticle modified carbon paste electrode was fabricated and used for study and sensitive determination of Direct Red 80 by cyclic voltammetry and differential pulse voltammetry. The overall analysis involved a two-step procedure: an accumulation step under open-circuit conditions, followed by voltammetric measurements of Direct Red 80 in a 0.1?M phosphate buffer solution at pH?=?3.0. The experimental conditions, such as the medium, pH and accumulation time, were optimised. The oxidation peak current was proportional to the concentration of Direct Red 80 from 5.0?×?10?8 to 5.0?×?10?7?M and 5.0?×?10?7 to 3.0?×?10?6?M, and the detection limit was 1.15?×?10?8?M (S/N?=?3). The proposed method was used to detect Direct Red 80 in natural water and sewage with good accuracy.  相似文献   
967.
Abstract

New metal complexes derived from the reaction of N-benzoyl-N′-carboxyl methylthiopropylidine thiourea (BCMT) with Cu(II), Co(II), Ni(II), and Fe(III) chloride and/or acetate salts have been synthesized and characterized using elemental analyses, molar conductance, spectral (IR, UV-Vis., mass, 1H NMR), thermal (TGA, DTG), and magnetic measurements. The IR results showed the modes of coordination in case of mononuclear and binuclear metal complexes. Different types of geometries are suggested on the basis of the spectral and the magnetic data. Also, the ligand field parameters for the metal complexes were calculated. The amounts of the solvents as well as the mechanism of decomposition were proposed using thermal measurements. The results of biological activity of the ligand give us the promise to be effective in tumors treatment.  相似文献   
968.
Layered double hydroxide (LDH)-based photocatalysts have emerged as a very promising candidate to replace TiO2, owing to their unique layered structure, tunable band gaps, low cost, ease of scale-up, and good photocatalytic activity. Bismuth-doped ZnCr-LDH was studied as photocatalyst in the photodegradation of methylene blue (MB). The structure and morphology of ZnCr-LDH and ZnCrBi-LDH were characterized using a different mode of delegated tools, e.g., FTIR, XRD, UV–Vis, FESEM–EDX, and TEM measurements. FESEM and TEM image of the synthesized LDHs showed that the synthesized LDH is smooth overlapping crystals, and they are approximately in hexagonal form. The material was found to be a good photocatalyst for degradation of methylene blue in visible light, and the results showed that the photocatalytic activity of ZnCrBi-LDH sample is higher than of ZnCr-LDH sample. According to the kinetic data, the reaction rate constant of ZnCrBi-LDH is approximately four times higher than the apparent reaction rate constant of ZnCr-LDH. The catalytic activity was retained even after four methylene blue degradation cycles, indicating that the LDH could be an important addition to the field of wastewater treatment.  相似文献   
969.
In-cuvette mixing and titration techniques have been used for the kinetic determination of sulfide based on its inhibition effect on the oxidation of indigo carmine with hexacyanoferrate(III) in the presence of silver. The reaction was monitored spectrophotometrically by measuring the decrease in absorbance of indigo carmine at 612 nm. Both initial rate and fixed-time methods were applied to the in-cuvette technique. Using in-cuvette mixing, sulfide up to 1800 ng was determined and detection limit and relative standard deviation for the determination of 120 ng of sulfide were calculated as 23.0 ng and 1.59%, respectively. On the basis of the titration technique, the upper limit of determination was 25 μg of sulfide and detection limit and average relative standard deviation for the determination of 1 μg of sulfide were 0.025 μg and 4.95%, respectively. The effect of foreign ions on the sulfide determination was studied. The proposed methods were applied to the determination of sulfide in water. Received: 10 March 1999 / Revised: 9 June 1999 / Accepted: 12 June 1999  相似文献   
970.
Reversible hybridization reaction plays a key role in fundamental biological processes, in many laboratory techniques, and also in DNA based sensing devices. Comprehensive investigation of this process is, therefore, essential for the development of more sophisticated applications. Kinetics and thermodynamics of the hybridization reaction, as a second order process, are systematically investigated with the aid of the soft and hard chemometric methods. Labeling two complementary 21 mer DNA single strands with FAM and Texas red fluorophores, enabled recording of the florescence excitation−emission matrices during the experiments which led to three-way data sets. The presence of fluorescence resonance energy transfer in excitation and emission modes and the closure in concentration mode, made the three-way data arrays rank deficient. To acquire primary chemical information, restricted Tucker3 as a soft method was employed. Herein a model-based method, hard restricted trilinear decomposition, is introduced for in depth analysis of rank deficient three-way data sets. By employing proposed hard method, the nonlinear model parameters as well as the correct profiles could be estimated. In addition, a simple constraint is presented to extract chemically reasonable output profiles regarding the core elements of restricted Tucker3 model.  相似文献   
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