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51.
Rashmin khanam Raj kumar Iram Iqbal Hejazi Syed Shahabuddin Ramovatar Meena Paulraj Rajamani Nitin Yadav Asif Iqbal Bhat Fareeda Athar 《Journal of cellular biochemistry》2019,120(2):1651-1666
N-benzhydrylpiperazine and 1,3,4-oxadiazoles are pharmacologically active scaffolds which exhibits significant inhibitory growth effects against various cancer cells, however, antiproliferation effects and the underlying mechanism for inducing apoptosis for aforementioned scaffolds addressing HeLa cancer cells remains uncertain. In this study, N-benzhydrylpiperazine clubbed with 1,3,4-oxadiazoles ( 4a–4h ) were synthesized, subsequently characterized using high resolution spectroscopic techniques and eventually evaluated for their antiproliferation potential by inducing apoptosis in HeLa cancer cells. The MTT assay screening results revealed that among all, compound 4d ( N-benzhydryl-4-((5-(4-aminophenyl)-1,3,4-oxadiazol-2-yl)methyl)piperazine) in particular, exhibited IC 50 value of 28.13 ± 0.21 μg/mL and significantly inhibited the proliferation of HeLa cancer cells in concentration-dependent manner. The in vitro anticancer assays for treated HeLa cells resulted in alterations in the cell morphology, reduction in colony formation, and inhibition of cell migration in concentration-dependent treatment. Furthermore, G2/M phase arrest, variations in the nuclear morphology, degradation of chromosomal DNA confirmed the ongoing apoptosis in treated HeLa cells. Increase in the expression of cytochrome C and caspase-3 confirmed the involvement of intrinsic mitochondrial pathway regulating the cell death. Also, elevation in reactive oxygen species level and loss of mitochondrial membrane potential signified that compound 4d induced apoptosis in HeLa cells by generating the oxidative stress. Therefore, compound 4d may act as a potent chemotherapeutic agent against human cervical cancer. 相似文献
52.
Rizwan Rasheed A. Wahid M. Farooq Iqbal Hussain Shahzad M. A. Basra 《Plant Growth Regulation》2011,65(1):35-45
High temperature strongly hampers the plant growth particularly at early growth stages. In this study, changes in some physiological
and anatomical characteristics and possibility of mitigating the adversities of heat stress by soaking sugarcane nodal buds
in 20 mM proline and glycinebetaine (GB) solutions have been explored. Heat stress reduced the rate of bud sprouting nonetheless
soaking the setts in proline followed by GB was beneficial. In addition, heat stress reduced the bud fresh and dry weights,
generated H2O2, reduced the tissue levels of K+ and Ca2+, while increased the osmolytes synthesis in a time course manner. Heat stress also delayed the emergence and expansion of
new bud leaves, by restricting the number and area of mesophyll cells. It also caused poor and aberrant development and diffused
appearance of mesophyll cells and vascular bundles in the bud leaves. However, soaking of buds in proline and GB solutions
substantially reduced the H2O2 production, improved the accumulation of soluble sugars and protected the developing tissues from heat stress effects; although
proline was more effective than GB. Correlations of various attributes indicated that soaking in GB and proline restricted
the H2O2 generation, improved K+ and Ca2+ contents, and increased the concentrations of free proline, GB and soluble sugars eventually improving the heat tolerance
of buds. Cost-benefit analysis showed that, considering increase in sprouting of buds, soaking in 20 mM solution of both osmoprotectants
is economical. 相似文献
53.
Nida Iram Muhammad Salahuddin Shah Fouzia Ismat Mudasser Habib Mazhar Iqbal S. Samar Hasnain Moazur Rahman 《Applied microbiology and biotechnology》2014,98(4):1691-1701
Newcastle disease virus (NDV) is an infectious agent of a large variety of birds, including chicken, which poses a real threat to the agriculture industry. Matrix (M) proteins of NDV and many other viruses perform critical functions during viral assembly and budding from the host cell. M-proteins are well conserved and therefore are potential targets for antiviral therapies. To validate this, we expressed the NDV M-protein in its native form in Saccharomyces cerevisiae and in inclusion bodies in Escherichia coli. Proper refolding of the recombinant protein produced in E. coli was verified using circular dichroism and infrared spectroscopies and electron microscopy. Immunization of chickens with the NDV M-protein elicited significant serum antibody titers. However, the antibodies conferred little protection against the ND following lethal viral challenges. We conclude that the M-protein is not exposed on the surface of the host cell or the virus at any stage during its life cycle. We discuss how the conserved M-protein can further be exploited as an antiviral drug target. 相似文献
54.
Khan Salman Khan Mukhtaj Iqbal Nadeem Hussain Tahir Khan Sher Afzal Chou Kuo-Chen 《International journal of peptide research and therapeutics》2020,26(2):795-809
International Journal of Peptide Research and Therapeutics - Piwi interacting RNA (piRNA) molecules belong to a largest class of small non coding RNA molecules which are originally discovered in... 相似文献
55.
Shah Y Iqbal Z Ahmad L Khan A Khan MI Nazir S Nasir F 《Journal of chromatography. B, Analytical technologies in the biomedical and life sciences》2011,879(9-10):557-563
A novel, precise, accurate and rapid isocratic reversed-phase high performance liquid chromatographic/ultraviolet (RP-HPLC/UV) method was developed, optimized and validated for simultaneous determination of rosuvastatin and atorvastatin in human serum using naproxen sodium as an internal standard. Effect of different experimental parameters and various particulate columns on the analysis of these analytes was evaluated. The method showed adequate separation for rosuvastatin and atorvastatin and best resolution was achieved with Brownlee analytical C18 column (150×4.6 mm, 5 μm) using methanol-water (68:32, v/v; pH adjusted to 3.0 with trifluoroacetic acid) as a mobile phase at a flow rate of 1.5 ml/min and wavelength of 241 nm. The calibration curves were linear over the concentration ranges of 2.0-256 ng/ml for rosuvastatin and 3.0-384 ng/ml for atorvastatin. The lower limit of detection (LLOD) and lower limit of quantification (LLOQ) for rosuvastatin were 0.6 and 2.0 ng/ml while for atorvastatin were 1.0 and 3.0ng/ml, respectively. All the analytes were separated in less than 7.0 min. The proposed method could be applied for routine laboratory analysis of rosuvastatin and atorvastatin in human serum samples, pharmaceutical formulations, drug-drug interaction studies and pharmacokinetics studies. 相似文献
56.
Takhi M Singh G Murugan C Thaplyyal N Maitra S Bhaskarreddy KM Amarnath PV Mallik A Harisudan T Trivedi RK Sreenivas K Selvakumar N Iqbal J 《Bioorganic & medicinal chemistry letters》2008,18(18):5150-5155
Novel oxazolidinone antibacterials bearing a variety of 3-indolylglyoxamide substituents have been explored in an effort to improve the spectrum and potency of this class of agents. A subclass of this series was also made with the diversity at C-5 terminus. These derivatives have been screened against a panel of clinically relevant Gram-positive pathogens and fastidious Gram-negative organisms. Several analogs in this series were identified with in vitro activity superior to linezolid (MIC=0.25-2 microg/mL). Compounds 10a, 10c, 10e and 10f displayed activity against linezolid resistant Gram-positive organisms (MIC=2-4 microg/mL). Selected oxazolidinones were evaluated for in vivo efficacy against a mouse systemic infection model. 相似文献
57.
58.
Pal C Bindu S Dey S Alam A Goyal M Iqbal MS Sarkar S Kumar R Halder KK Debnath MC Adhikari S Bandyopadhyay U 《The Journal of biological chemistry》2012,287(5):3495-3509
We have investigated the gastroprotective effect of SEGA (3a), a newly synthesized tryptamine-gallic acid hybrid molecule against non-steroidal anti-inflammatory drug (NSAID)-induced gastropathy with mechanistic details. SEGA (3a) prevents indomethacin (NSAID)-induced mitochondrial oxidative stress (MOS) and dysfunctions in gastric mucosal cells, which play a pathogenic role in inducing gastropathy. SEGA (3a) offers this mitoprotective effect by scavenging of mitochondrial superoxide anion (O(2)(·-)) and intramitochondrial free iron released as a result of MOS. SEGA (3a) in vivo blocks indomethacin-mediated MOS, as is evident from the inhibition of indomethacin-induced mitochondrial protein carbonyl formation, lipid peroxidation, and thiol depletion. SEGA (3a) corrects indomethacin-mediated mitochondrial dysfunction in vivo by restoring defective electron transport chain function, collapse of transmembrane potential, and loss of dehydrogenase activity. SEGA (3a) not only corrects mitochondrial dysfunction but also inhibits the activation of the mitochondrial pathway of apoptosis by indomethacin. SEGA (3a) inhibits indomethacin-induced down-regulation of bcl-2 and up-regulation of bax genes in gastric mucosa. SEGA (3a) also inhibits indometacin-induced activation of caspase-9 and caspase-3 in gastric mucosa. Besides the gastroprotective effect against NSAID, SEGA (3a) also expedites the healing of already damaged gastric mucosa. Radiolabeled ((99m)Tc-labeled SEGA (3a)) tracer studies confirm that SEGA (3a) enters into mitochondria of gastric mucosal cell in vivo, and it is quite stable in serum. Thus, SEGA (3a) bears an immense potential to be a novel gastroprotective agent against NSAID-induced gastropathy. 相似文献
59.
Naeem lqbal Muhammad Yasin Ashraf Farrukh Javed Muhammad Ashmf Sohail Hameed 《植物学报(英文版)》2006,48(5):558-562
In the present study, the relationship between the nutritional status of leaves and the development of symptoms of cotton leaf curl virus (CLCuV) in two cotton (Gossypium hirsutum L.) cuItlvars (I.e. CIM-240 and S-12) was Investigated. The incidence of disease attack was found to be 100% In the S-12 cuItlvar and 16% in the CIM-240 cuItivar. Geminivirus particles in infected leaves were confirmed by transmission electron microscope examination of highly specific geminivirus coat protein antlsera-treated cell sap. The CLCuV Impaired the accumulation of different nutrients in both cuItivars. A marked decrease in the accumulation of Ca^2+ and K^+ was observed in infected leaves. However, the disease had no effect on leaf concentrations of Na^+, N, and P. It was observed that the curling of leaf margins in CLCuV-Infected plants was associated with the leaf Ca^2+ content; leaf curling was severe in plants with a significant reduction In Ca^2+ content. Moreover, leaf K&+ content was found to be associated with resistance/susceptibility to CLCuV infection. 相似文献
60.
Humayun Pervez Mohammad S. Iqbal Muhammad Younas Tahir Faiz-ul-Hassan Nasim Muhammad Iqbal Choudhary Khalid Mohammed Khan 《Journal of enzyme inhibition and medicinal chemistry》2013,28(6):848-854
A series of 15 previously reported N4-substituted isatin-3-thiosemicarbazones 3a-o has been screened for cytotoxic, antibacterial, antifungal and urease inhibitory activities. Compounds 3b, 3e and 3n proved to be active in cytotoxicity assay; 3e exhibited a high degree of cytotoxic activity (LD50 = 1.10 × 10? 5 M). Compound 3h exhibited significant antibacterial activity against B. subtilis, whereas compounds 3a, 3k and 3l displayed significant antifungal activity against one or more fungal strains i.e. T. longifusus, A. flavus and M. canis. In human urease enzyme inhibition assay, compounds 3g, 3k and 3m proved to be the most potent inhibitors, exhibiting relatively pronounced inhibition of the enzyme. These compounds, being non-toxic, could be potential candidates for orally effective therapeutic agents to treat certain clinical conditions induced by bacterial ureases like H. pylori urease. This study presents the first example of inhibition of urease by isatin-thiosemicarbazones and as such provides a solid basis for further research on such compounds to develop more potent inhibitors. 相似文献