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排序方式: 共有1327条查询结果,搜索用时 312 毫秒
1.
In this paper, we have established methylenebis (4-hydroxy-2H-chromen-2-one) as a promising anticancer scaffold with kinesin spindle protein (KSP) inhibitory activity under malignant condition. A series of biscoumarin derivatives (MN1 to MN30) with different substituent were synthesized, and their anticancer activity was explored. Six biscoumarin derivatives that were found active were further selected to formulate organic nanoparticles (ONPs). Anticancer activity of both the forms (viz conventional and ONPs) was compared. MN30 was found most potent whereby MN10 showed good anticancer activity in both, i.e., conventional and ONP form; the structural activity relationship (SAR) study has been established. Computational investigation revealed biscoumarin scaffold as a suitable pharmacophore to bind against KSP protein. Molecular dynamics simulation studies revealed protein-ligand stability and dynamic behavior of biscoumarin-KSP complex. Finally, accruing signal transduction model was formulated to explain the observed MTT trend of conventional and ONP form. The model seems useful towards solving population specific varied results of chemotherapeutic agents. According to the model, MN10 and MN30 derivatives have good pharmacodynamics inertia and therefore, both the molecules were able to provide dose-dependent cytotoxic results. 相似文献
2.
SINGLE MACHINE SCHEDULING WITH CONTROLLABLE PROCESSING TIMES AND COMPRESSION COSTS (PART I:EQUAL TIMES AND COSTS) 总被引:1,自引:0,他引:1
Most papers in scheduling research have treated individual job processing times as fixed parameters. However, in many practical situations, a manager may control processing time by realloeating resources. In this paper, authors consider a machine scheduling problemwith controllable processing times. In the first part of this paper, a special case where the pro-cessing times and compression costs are uniform among jobs is discussed. Theoretical results are derived that aid in developing an O(n^2) algorithm to slove the problem optimally. In the second part of this paper, authors generalize the discussion to general case, An effective heuristic to the genera/ problem will be presented. 相似文献
3.
2,5-二[2′-(4′-氯代苯氧乙酸)基]-1,3,4-噻二唑的合成 总被引:2,自引:0,他引:2
通过对称双酰肼与P_2S_5的缩合反应合成2,5-二-羟苯基-1,3,4-噻二唑,并由此制备了2,5-二[2′-(4′-氯代苯氧乙酸)基]-1,3,4-噻二唑及其相关化合物,同时测定了它们的生物活性。 相似文献
4.
α-(1H-1,2,4-三唑-1-基)-β-芳硫基取代苯酮的合成及生物活性研究 总被引:1,自引:0,他引:1
利用 2 (1H 1,2 ,4 三唑 1 基 ) 2 丙烯 1 酮 (2 )与取代硫酚或含巯基的杂环化合物进行 1,4 亲核加成 ,得到目标化合物 3,其结构经元素分析、核磁和红外光谱所证实 ,并对其进行了生物活性的测试 ,发现大部分化合物具有很好的抑菌活性 .结构与活性的关系表明不同的R1取代对其生物活性有较大的影响 ,当R1=(CH3 ) 3 C时 ,对小麦锈病的抑制活性要高于R1=Ar的活性 ,而Ar上不同的取代基对其活性影响不大 相似文献
5.
Mohamed Shaaban Marwa Y. Issa Mohamed A. Ghani Abdelaaty Hamed Ahmed B. Abdelwahab 《Natural product research》2019,33(1):24-33
During our continual searching programme for novel bioactive metabolites from Sarcophyton trocheliophorum, collected from Red Sea, we describe herein the isolation and structural elucidation of further two new pyrane-based cembranoid diterpenes: 9-hydroxy-7,8-dehydro-sarcotrocheliol (1) and 8,9-expoy-sarcotrocheliol acetate (2), along with the well-known sarcotrocheliol acetate (3), (+)-sarcophine (4), (+)-sarcophytoxide (5) and (-)-sarcophytoxide (6). The chemical structures of compounds 1 and 2 were determined on the basis of 1D and 2D NMR (1H, 13C, 1H–1H COSY, HMQC, HMBC and NOE), mass spectra (ESI and HR-ESIMS) and by comparison with related structures. The antimicrobial activities of the reported compounds 1–6 were investigated. According to the molecular docking study of compounds 1–6 using 3D structure of α,β tubulin in complex with taxol (PDB code 1JFF) and epothilone A (PDB code 1TVK), sarcophine (4) displayed the highest affinity towards both crystal structures, followed by 5 and 6, meanwhile pyrane-based cembranoid diterpenes (1–3) showed less affinity. 相似文献
6.
Helmut Spreitzer Edith Rodinger Andrea Pichler Gerhard Buchbauer 《Monatshefte für Chemie / Chemical Monthly》1990,121(11):955-961
Summary The bicyclo[2.2.1]- and [2.2.2]-systems are part of numerous biological active substances. Continuing our syntheses in the isocamphane series the homologous isocamphanes of mecamylamine (1 a) and of the fungicidal bicyclic compound2 were synthesized. Furthermore the syntheses ofE-homoisosantalene (15) andE,E-homoisosantalol (16) are described. 相似文献
7.
利用N,N-二(2-氯乙基)氨基磷酰二异氰酸酯和胺的加成反应,合成了2,4,6三氧-1,3,5,2三氮磷杂环己烷衍生物,它们的结构经^1HNMR,IR和元素分析所证实。初步生物活性测试结果表明,部分化合物具有一定的抗肿瘤活性。 相似文献
8.
含钼化合物及其配合物的抗癌抗肿瘤活性 总被引:4,自引:0,他引:4
钼是生命体所必需的微量元素。本文介绍了钼在人体中的作用,钼缺乏和钼过量对人体的影响,并介绍了含钼化合物以及配合物的抗癌抗肿瘤研究情况。 相似文献
9.
本文报道了O-烷基-O-(2′-甲酰缩氨基硫脲苯基)-N-烷基硫代磷酰胺类化合物的合成方法,化合物3c和3e具有良好的除草活性。 相似文献
10.
Buneva VN Kanyshkova TG Vlassov AV Semenov DV Khlimankov DYu Breusova LR Nevinsky GA 《Applied biochemistry and biotechnology》1998,75(1):63-76
Various catalytically active antibodies (Abs), or abzymes, have been detected recently in the sera of patients with autoimmune
pathologies, in whom their presence is probably associated with autoimmunization. Normal humans are generally not considered
to have abzymes, since no obvious immunizing factors are present. Here is shown by different methods that IgG from the milk
of normal females possesses both DNase and RNase activities. The activities were also present in the IgG F(ab′)2 and Fab fragments.
Affinity modification of IgG by the chemically reactive derivative of an oligonucleotide led to preferential modification
of the L chain of IgG. After separation of the subunits by sodium dodecyl sulfate electrophoresis in a gel containing DNA,
an in-gel assay showed DNase activity in the L chain. The L chain separated by affinity chromatography on DNA-cellulose was
catalytically active. These findings speak in favor of the generation of cat alytic Abs by the immune system of healthy mothers.
It is known that the treatment of adults with DNases and RNases offers protection from viral and bacterial diseases. Since
breast milk protects the infants from infec tions until the immune system is developed, this raises the possibility that catalytic
Abs like nucleases, may possess a protective role. 相似文献