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131.
Raymond Wai‐Yin Sun Dr. Carrie Ka‐Lei Li Dr. Dik‐Lung Ma Dr. Jessie Jing Yan Chun‐Nam Lok Dr. Chung‐Hang Leung Dr. Nianyong Zhu Dr. Chi‐Ming Che Prof. Dr. 《Chemistry (Weinheim an der Bergstrasse, Germany)》2010,16(10):3097-3113
In the design of physiologically stable anticancer gold(III) complexes, we have employed strongly chelating porphyrinato ligands to stabilize a gold(III) ion [Chem. Commun. 2003 , 1718; Coord. Chem. Rev. 2009 , 253, 1682]. In this work, a family of gold(III) tetraarylporphyrins with porphyrinato ligands containing different peripheral substituents on the meso‐aryl rings were prepared, and these complexes were used to study the structure–bioactivity relationship. The cytotoxic IC50 values of [Au(Por)]+ (Por=porphyrinato ligand), which range from 0.033 to >100 μM , correlate with their lipophilicity and cellular uptake. Some of them induce apoptosis and display preferential cytotoxicity toward cancer cells than to normal noncancerous cells. A new gold(III)–porphyrin with saccharide conjugation [Au(4‐glucosyl‐TPP)]Cl ( 2 a ; H2(4‐glucosyl‐TPP)=meso‐tetrakis(4‐β‐D ‐glucosylphenyl)porphyrin) exhibits significant cytostatic activity to cancer cells (IC50=1.2–9.0 μM ) without causing cell death and is much less toxic to lung fibroblast cells (IC50>100 μM ). The gold(III)–porphyrin complexes induce S‐phase cell‐cycle arrest of cancer cells as indicated by flow cytometric analysis, suggesting that the anticancer activity may be, in part, due to termination of DNA replication. The gold(III)–porphyrin complexes can bind to DNA in vitro with binding constants in the range of 4.9×105 to 4.1×106 dm3 mol?1 as determined by absorption titration. Complexes 2 a and [Au(TMPyP)]Cl5 ( 4 a ; [H2TMPyP]4+=meso‐tetrakis(N‐methylpyridinium‐4‐yl)porphyrin) interact with DNA in a manner similar to the DNA intercalator ethidium bromide as revealed by gel mobility shift assays and viscosity measurements. Both of them also inhibited the topoisomerase I induced relaxation of supercoiled DNA. Complex 4 a , a gold(III) derivative of the known G‐quadruplex‐interactive porphyrin [H2TMPyP]4+, can similarly inhibit the amplification of a DNA substrate containing G‐quadruplex structures in a polymerase chain reaction stop assay. In contrast to these reported complexes, complex 2 a and the parental gold(III)–porphyrin 1 a do not display a significant inhibitory effect (<10 %) on telomerase. Based on the results of protein expression analysis and computational docking experiments, the anti‐apoptotic bcl‐2 protein is a potential target for those gold(III)–porphyrin complexes with apoptosis‐inducing properties. Complex 2 a also displays prominent anti‐angiogenic properties in vitro. Taken together, the enhanced stabilization of the gold(III) ion and the ease of structural modification render porphyrins an attractive ligand system in the development of physiologically stable gold(III) complexes with anticancer and anti‐angiogenic activities. 相似文献
132.
133.
Journal of Statistical Physics - 相似文献
134.
The time averaged frame subtraction technique is improved by subtracting two Bessel fringe patterns at two different force levels. The technique enables significant enhancement of fringe contrast and increased measurement sensitivity. The contrast and sensitivity of the fringes obtained at different force ratios are investigated. Both theoretical and experimental results are presented. 相似文献
135.
The classical economic production quantity (EPQ) model assumes that items are produced by a perfectly reliable production process with a fixed set-up cost. While the reliability of the production process cannot be perfected cost-free, the set-up cost can be reduced by investment in flexibility improvement. In this paper, we propose an EPQ model with a flexible and imperfect production process. We formulate this inventory decision problem using geometric programming (GP), establish more general results using the arithmetic-geometric mean inequality, and solve the problem to obtain a closed-form optimal solution. Following the theoretical treatment, we provide a numerical example to demonstrate that GP has potential as a valuable analytical tool for studying a certain class of inventory control problems. Finally we discuss some aspects of sensitivity analysis of the optimal solution based on the GP approach. 相似文献
136.
O. Yavas P. Leiderer H. K. Park C. P. Grigoropoulos C. C. Poon W. P. Leung N. Do A. C. Tam 《Applied Physics A: Materials Science & Processing》1994,58(4):407-415
The dynamics of liquid-vapor phase-change in the nanosecond time-scale induced by pulsed-laser heating of a liquid on a solid sample is studied by means of optical reflectance and scattering measurements, and the piezoelectric detection technique. The liquids studied include water, ethanol, methanol, IsoproPropyl Alcohol (IPA), and mixtures of water and IPA. The threshold fluence for nucleation is determined with high accuracy using the optical and acoustic signals. Heat diffusion calculations performed for the threshold fluences indicate that the liquids are sufficiently superheated before nucleation sets on. The transient optical reflectance signal is analyzed by an effective-medium theory to provide bubble-growth kinetics, so that the bubble-growth velocity for the test liquids could be estimated. In addition, it is observed that, following the thermally induced nucleation, repetitive acoustic cavitation at the surface of the solid sample occurs, with a time interval related to the speed of sound in the liquid. 相似文献
137.
138.
Feiyue He Anthony Leung Srdjan Stojanovic 《Mathematical Methods in the Applied Sciences》1995,18(2):127-146
This paper considers the optimal harvesting control of a biological species, whose growth is governed by the parabolic diffusive Volterra-Lotka equation. We prove that such equation with L∞ periodic coefficients has an unique positive periodic solution. We show the existence and uniqueness of an optimal control, and under certain conditions, we characterize the optimal control in terms of a parabolic optimality system. A monotone sequence which converges to the optimal control is constructed. 相似文献
139.
This article considers the fluid model for the discharge of plasma particle species in display technology. The fluid equations are coupled with Poisson's equation, which describes the effect of the charged particles on the electric field. The diffusion and mobility coefficients for the positive ion particles depend on the electric field, while those for the electrons depend on the electron mean energy. The reaction rates are proportional to the products of the densities of the reacting particles involved in the particular ionization, conversion or recombination reactions. Moreover, the ionization coefficients are dependent on the electric field, which varies spatially and temporally. The main ionization and discharge reactions are described by an initial-boundary value problem for a system of coupled parabolic–elliptic partial differential equations. The system is first analyzed by upper–lower solution method. By means of the a priori bounds obtained for an arbitrary time, the existence of solution for the initial-boundary value problem is proved in an appropriate Hölder space. 相似文献
140.
The effect of non-linear magnetic forces on the non-linear response of the shaft is examined for the case of superharmonic resonance in this paper. It is shown that the steady-state superharmonic periodic solutions lose their stability by either saddle-node or Hopf bifurcations. The system exhibits many typical characteristics of the behavior of non-linear dynamical systems such as multiple coexisting solutions, jump phenomenon, and sensitive dependence on initial conditions. The effects of the feedback gains and imbalance eccentricity on the non-linear response of the system are studied. Finally, numerical simulations are performed to verify the analytical predictions. 相似文献