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61.
62.
    
The extensive development of radiopharmaceuticals towards early tumour detection and treatment has increased the demand for new ligands with higher tumour selectivity. Research has been done on the potential of the novel O,O′‐diethylethylenediamine‐N,N′‐di‐3‐propanoate ( L ) ligand as a radionuclide vehicle for tumour targeting. Under alkaline conditions, L hydrolyses and produces half ester ligand ( L' ) and diacid ligand ( L'' ), with characteristic donor atom array N,N,O. Ligand L was successfully labelled with 99mTc at pH = 9 by coordination with the octahedral fac‐[99mTc(CO)3(H2O)3]+ intermediate, forming the main radioproduct fac‐[99mTcL′(CO)3] (Tc1). The 99mTc complex showed a low lipophilic character (log P = 0.48) and low binding affinity to human serum albumin (2.51 ± 0.48%). In vitro stability studies in saline and human plasma, as well as challenge studies with cysteine and histidine, revealed high stability of the complex during 24 h. Biodistribution studies of Tc1 in female C57BL/6 mice bearing B16/F1 melanoma metastases showed significant tumour uptake: 9.81 ± 1.19%ID g?1 in the liver, 5.87 ± 0.54%ID g?1 in the lungs and 3.17 ± 0.33%ID g?1 in the ovary at 30 min post‐injection. Favourable physicochemical properties, satisfactory in vitro/in vivo stability and biodistribution profile in the experimental metastatic melanoma model indicate the possible application of the radiolabelled ligand in tumour diagnosis. Copyright © 2015 John Wiley & Sons, Ltd.  相似文献   
63.
In this paper we consider a class of toroids generated by a meridian in a shape of quadrangle in an arbitrary position to the axis of revolution.We give geometrical meaning of the non-rigidity condition based on the position of the diagonals of meridian. Special classes of quadrangular meridians (trapezium, parallelogram, deltoid, … ) are discussed. The number of flexible toroids is considered. A tool SurfBend is developed for the rigidity and visualization.  相似文献   
64.
In this paper we define generalized Kählerian spaces of the first kind (\(G_1^K N\)) given by (2.1)–(2.3). For them we consider hollomorphically projective mappings with invariant complex structure. Also, we consider equitorsion geodesic mapping between these two spaces (\(G_1^K N\) and \(G_1^{\bar K} N\)) and for them we find invariant geometric objects.  相似文献   
65.
66.
    
We consider the double field formulation of the closed bosonic string theory, and calculate the Poisson bracket algebra of the symmetry generators governing both general coordinate and local gauge transformations. Parameters of both of these symmetries depend on a double coordinate, defined as a direct sum of the initial and T-dual coordinate. When no antisymmetric field is present, the C-bracket appears as the Lie bracket generalization in a double theory. With the introduction of the Kalb-Ramond field, the B-twisted C-bracket appears, while with the introduction of the non-commutativity parameter, the θ-twisted C-bracket appears. We present the derivation of these brackets and comment on their relations to analogous twisted Courant brackets and T-duality.  相似文献   
67.
The fourth order nonlinear differential equations A with regularly varying coefficient q(t) are studied in the framework of regular variation. It is shown that thorough and complete information can be acquired about the existence of all possible regularly varying solutions of (A) and their accurate asymptotic behavior at infinity.  相似文献   
68.

Background  

In microorganisms and plants, the first two reactions of arginine biosynthesis are catalyzed by N-acetylglutamate synthase (NAGS) and N-acetylglutamate kinase (NAGK). In mammals, NAGS produces an essential activator of carbamylphosphate synthetase I, the first enzyme of the urea cycle, and no functional NAGK homolog has been found. Unlike the other urea cycle enzymes, whose bacterial counterparts could be readily identified by their sequence conservation with arginine biosynthetic enzymes, mammalian NAGS gene was very divergent, making it the last urea cycle gene to be discovered. Limited sequence similarity between E. coli NAGS and fungal NAGK suggests that bacterial and eukaryotic NAGS, and fungal NAGK arose from the fusion of genes encoding an ancestral NAGK (argB) and an acetyltransferase. However, mammalian NAGS no longer retains any NAGK catalytic activity.  相似文献   
69.
The crystal structure of the title compound has been determined from 6049 X-ray diffractometric intensities with I > 3σ(I), and refined by a least-squares procedure to R = 0.050. The crystals are monoclinic, space group P21/n, a = 13.702(2) b = 14.255(2), c = 39.556(6) Å, β = 94.75(1)°, Z = 4. The structure of the cation displays two different coordination modes of the Ph2PCH2PPh2 ligands. Two of these are bidentate, bridging the Pt-Pt bond [2.769(1)Å] to form a Pt2(μ-Ph2PCH2PPh2)2 nucleus, while the third acts as a monodentate two-electron donor. The hydrido ligand was not located, but its position is inferred from the coordination geometry of the platinum atom to which it is bonded. The metalligand distances are: Pt-P(trans to P) 2.248(3)–2.289(4) and Pt—P(trans to Pt) 2.347(4) Å.  相似文献   
70.
ABSTRACT

A synthesis of two series of 3-substituted quinazolinones was performed utilizing a green chemistry approach, deep eutectic solvents and microwaves, namely. 2-Methyl-3-substituted-quinazolin-4(3H)-one derivatives were synthesized in a two-step reaction, using choline chloride:urea deep eutectic solvent (DES). 3-Substituted-quinazolin-4(3H)-ones were synthesized in one-pot one-step reaction of anthranilic acid, amines and orthoester in a microwave reactor. For the synthesis of 2-methyl-3-substituted-quinazolin-4(3H)-ones, first conventional synthesis of benzoxazinone, as an intermediate, was performed. Further, benzoxazinone in reaction with corresponding amines, in choline choline:urea deep eutectic solvent, furnished desired compounds. These procedures are based on green principles with the aim of developing synthetic routes for the potential antitumor agents. All compounds were characterized by LC/MS, 1H NMR and 13C NMR spectral techniques. Compound 1 bearing trifluoromethoxyphenyl group showed promising activity against HuT-78 cell line with IC50 of 51.4?±?5.1?µM.  相似文献   
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