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141.
Hendrik Schneider Lukas Deweid Thomas Pirzer Desislava Yanakieva Simon Englert Bastian Becker Dr. Olga Avrutina Prof. Dr. Harald Kolmar 《ChemistryOpen》2019,8(3):354-357
Antibody-drug conjugates (ADCs) are multicomponent biomolecules that have emerged as a powerful tool for targeted tumor therapy. Combining specific binding of an immunoglobulin with toxic properties of a payload, they however often suffer from poor hydrophilicity when loaded with a high amount of toxins. To address these issues simultaneously, we developed dextramabs, a novel class of hybrid antibody-drug conjugates. In these architectures, the therapeutic antibody trastuzumab is equipped with a multivalent dextran polysaccharide that enables efficient loading with a potent toxin in a controllable fashion. Our modular chemoenzymatic approach provides an access to synthetic dextramabs bearing monomethyl auristatin as releasable cytotoxic cargo. They possess high drug-to-antibody ratios, remarkable hydrophilicity, and high toxicity in vitro. 相似文献
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Analytical and Bioanalytical Chemistry - 相似文献
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147.
A collection of the cyanobacterium Lyngbya confervoides off Grassy Key in Florida yielded grassypeptolide (1), a 31-membered macrocyclic depsipeptide with unusually high D-amino acid content, two thiazolines, and one beta-amino acid. We report the rigorous 3D structure determination and conformational analysis in solution and solid state by NMR, MS, X-ray crystallography, chemical degradation, and molecular modeling involving distance geometry and restrained molecular dynamics. Grassypeptolide (1) inhibited cancer cell growth with IC50 values from 1.0 to 4.2 microM. 相似文献
148.
Amarie S Arefe K Starcke JH Dreuw A Wachtveitl J 《The journal of physical chemistry. B》2008,112(44):14011-14017
Carotenoids are the crucial pigments involved in photoprotection and in scavenging harmful free radicals in all living organisms. The underlying chemical processes are charge transfer and free radical reactions, both of them leading to carotenoid radical cation (Car*+) formation. Accurate knowledge of the molecular properties of Car*+ is thus a prerequisite for understanding of their function as photoprotective and antioxidant agents. Despite their fundamental importance in nonphotochemical quenching in green plants, only little is known about the Car*+ excited states and their dynamics. Our combined experimental and theoretical investigation employing femtosecond time-resolved pump-probe spectroscopy and quantum chemical calculations proves the existence of a second low-lying pipi* excited-state energetically below the well-known strongly allowed excited-state responsible for the intense absorption of Car*+ in the near-IR region. Hence, we suggest denoting the latter state as D3 state in the future. Our findings have also implications for nonphotochemical quenching in green plants, since direct quenching of chlorophyll excited states by Forster energy transfer to Car*+ is possible and efficient. 相似文献
149.
Lie ZS Pardede M Hedwig R Suliyanti MM Kurniawan KH Munadi Lee YI Kagawa K Hattori I Tjia MO 《Analytical and bioanalytical chemistry》2008,390(7):1781-1787
The applicability of spectrochemical analysis of minute amounts of powder samples was investigated using an ultraviolet Nd-YAG
laser (355 nm) and low-pressure ambient air. A large variety of chemical powder samples of different composition were employed
in the experiment. These included a mixture of copper(II) sulfate pentahydrate, zinc sulfide, and chromium(III) sulfate n-hydrate powders, baby powder, cosmetic powders, gold films, zinc supplement tablet, and muds and soils from different areas.
The powder samples were prepared by pulverizing the original samples to an average size of around 30 μm in order to trap them
in the tiny micro holes created on the surface of the quartz subtarget. It was demonstrated that in all cases studied, good
quality spectra were obtained with low background, free from undesirable contamination by the subtarget elements and featuring
ppm sensitivity. A further measurement revealed a linear calibration curve with zero intercept. These results clearly show
the potential application of this technique for practical qualitative and quantitative spectrochemical analysis of powder
samples in various fields of study and investigation. 相似文献
150.
The standard C∗-algebraic version of the algebra of canonical commutation relations, the Weyl algebra, frequently causes difficulties in applications since it neither admits the formulation of physically interesting dynamical laws nor does it incorporate pertinent physical observables such as (bounded functions of) the Hamiltonian. Here a novel C∗-algebra of the canonical commutation relations is presented which does not suffer from such problems. It is based on the resolvents of the canonical operators and their algebraic relations. The resulting C∗-algebra, the resolvent algebra, is shown to have many desirable analytic properties and the regularity structure of its representations is surprisingly simple. Moreover, the resolvent algebra is a convenient framework for applications to interacting and to constrained quantum systems, as we demonstrate by several examples. 相似文献