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Increase in the number of infections caused by pathogenic microbes in cancer patients has prompted the searcher to invest in the development of agents having dual anticancer and antimicrobial properties. The present study is concerned with synthesis and screening for anticancer and antimicrobial activity of a series of 5-hydrazinyl-2-(2-(1-(thien-2-yl)ethylidene)hydrazinyl)thiazole derivatives. The structure elucidation of the synthesized hydrazinyl thiazole derivatives was illustrated by spectroscopic and elemental analysis. All the newly synthesized compounds 5a-p were evaluated for in-vitro cytotoxic activity against breast carcinoma (MCF-7 cell line), hepatocellular carcinoma (HePG-2) and colorectal cancer (HCT-116) cell lines using MTT assay method. Compounds 5 g, 5h showed broad spectrum activity against three cancer cell lines with IC50 ranged from 3.81 to 11.34 µM in compared to the reference drug Roscovitine (IC50 = 9.32 to 13.82 µM), while compounds 5 l and 5 m were found to be more selective against HePG-2 and HCT-116 cell line (IC50 = 9.29 and 8.93 µM respectively) and compound 5j was more selective against HePG-2 and MCF-7 cell lines (IC50 = 6.73 and 10.87 µM respectively). The inhibitory activity of the most promising compounds was tested against the EGFR and ARO enzymes and were further tested for apoptosis and Annexin V/PI staining. The results of enzyme-based tests revealed that the tested compound 5j has a dual inhibitory effect on the EGFR and ARO enzymes with IC50 = 82.8 and 98.6 nM respectively in compared to the reference drugs Erlotinib and Letrozole (IC50 = 62.4 and 79 nM respectively). Furthermore, the majority of the tested hydrazinyl thiazole derivatives exhibited significant antimicrobial activity against the used pathogenic microbes species. Compounds 4b, 5h, 5j and 5 m exerted a good antibacterial and antifungal activity against all tested pathogenic microbes. Therefore, it was concluded that compounds 5 h, 5j and 5 m proved to possess dual anticancer and antimicrobial agent and may serves as a useful lead compounds in search for further modification or derivatization to give more potent and selective agents.  相似文献   
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BackgroundNasopharyngeal cancer is a tumor that occurs in the mucous epithelium of the nasopharynx. Due to its rapid growth and early metastatic nature, the successful treatment of nasopharyngeal cancer is highly challenging.ObjectiveHere, we intended to assess the in vitro anticancer property of brassinin against the nasopharyngeal cancer C666-1 cells.MethodologyThe in vitro free radical scavenging property of the brassinin was assessed by various free radical scavenging activities such as FRAP, DPPH, chemiluminescence (CL), and ORAC assays. The cytotoxic level of the brassinin (1–50 µM) against the nasopharyngeal cancer C666-1 cells and normal Vero cells were assessed by the MTT cytotoxicity assay. The levels of TBARS, GSH, and the SOD activity was assessed using kits. The level of ROS generation, MMP, and apoptosis were investigated by the respective fluorescent staining techniques. The flow cytometry analysis was done to scrutinize the cell cycle arrest. The Bax/Bcl-2 level and caspase activities were examined using respective kits.ResultsThe brassinin treatment effectively scavenged the free radicals, which are assessed by the FRAP, DPPH, chemiluminescence (CL), and ORAC assays. The proliferation of brassinin treated C666-1 cells were decreased remarkably, while the same concentration of brassinin did not disturbed the Vero cell viability. The 30 µM of brassinin effectively increased the ROS production, depleted the MMP, and stimulated the apoptosis in the C666-1 cells. The brassinin increased the TBARS and depleted the GSH and SOD in the C666-1 cells. The flow cytometry analysis revealed that the brassinin administration improved the G0/G1 ratio and decreased the proportion of cells with ‘S’ and ‘G2/M’ phase. The Bax, caspase-3 and ?9 were elevated and Bcl-2 level was decreased in the brassinin administered C666-1 cells.ConclusionOur findings discovered that the brassinin has the capacity to prevent the proliferation and stimulate the apoptotic cell death C666‐1 cells via blocking cell cycle and increasing oxidative stress and apoptotic markers. Hence, it can be a talented therapeutic agent to treat the nasopharyngeal cancer in the future.  相似文献   
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卜月华  张恒 《运筹学学报》2022,26(2):111-127
$G$的强边染色是在正常边染色的基础上, 要求距离不超过$2$的任意两条边染不同的颜色, 强边染色所用颜色的最小整数称为图$G$的强边色数。本文首先给出极小反例的构型, 然后通过权转移法, 证明了$g(G)\geq5$, $\Delta(G)\geq6$$5$-圈不相交的平面图的强边色数至多是$4\Delta(G)-1$。  相似文献   
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食管鳞状细胞癌(ESCC)患者发病早期由于体内的肿瘤标志物种类少且含量低,难以在患病早期发现疾病从而快速反应并有效治疗。因此,找到一种合适的标志物对其进行快速高效检测是研究者亟待解决的问题。血小板衍生生长因子(PDGF-BB)在恶性肿瘤的早期诊断中具有极其重要的地位。该文基于酶循环放大荧光光谱设计了一种用于PDGF-BB检测的DNA生物传感器,利用特定位点剪切酶,实现了信号放大,检出限由1 fmol/L降至1 amol/L,大大提高了检测的灵敏度。该方法通过检测血液中PDGF-BB浓度,从而实现对ESCC的简单、快速、高效诊断,在生物化学和医学应用上具有重要价值。  相似文献   
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We discuss the length of the longest directed cycle in the sparse random digraph , constant. We show that for large there exists a function such that a.s. The function where is a polynomial in . We are only able to explicitly give the values , although we could in principle compute any .  相似文献   
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热再生吸收式碳捕集的传统认识难以揭示其热力学机制,一种新的认识是"热-化学能"转换中存在中间能量形式。本文从热力学碳泵概念出发,对吸收式碳捕集理想系统进行了解耦,其可视为"热机-碳泵"的热力学组合,探索了极限效率的表达,并采用第二定律效率作为评价参数对已有中试试验系统进行了性能水平探索。结果表明,理想循环性能系数仅取决于热源汇温度、碳源汇浓度;中试系统第二定律效率普遍低于20%。本文探索了热驱动的吸收式碳捕集热力学机制,为新型吸收剂设计提供了新思路。  相似文献   
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《Discrete Mathematics》2022,345(12):113069
The toughness of a noncomplete graph G is the maximum real number t such that the ratio of |S| to the number of components of G?S is at least t for every cutset S of G. Determining the toughness for a given graph is NP-hard. Chvátal's toughness conjecture, stating that there exists a constant t0 such that every graph with toughness at least t0 is hamiltonian, is still open for general graphs. A graph is called (P32P1)-free if it does not contain any induced subgraph isomorphic to P32P1, the disjoint union of P3 and two isolated vertices. In this paper, we confirm Chvátal's toughness conjecture for (P32P1)-free graphs by showing that every 7-tough (P32P1)-free graph on at least three vertices is hamiltonian.  相似文献   
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《Discrete Mathematics》2022,345(10):113028
We prove that every 52-connected line graph of a rank 3 hypergraph is Hamiltonian. This is the first result of this type for hypergraphs of bounded rank other than ordinary graphs.  相似文献   
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