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81.
Systems biology needs to show practical relevance to commercial biological challenges such as those of pharmaceutical development. The aim of this work is to design and validate some applications in anti-cancer therapeutic development. The test system was a group of novel cyclin-dependent kinase (CDK) inhibitors synthesised by Cyclacel Ltd. The measured in vitro IC50s of each compound were used as input data to a proprietary cell cycle model developed by Physiomics plc. The model was able to predict over three orders of magnitude the cytotoxicity of each compound without model adaptation to specific cancer cell types. This pattern matched the experimentally determined data. One class of compounds was predicted to cause an increase of the cell cycle length with a non-linear dose-response curve. Further work will use apoptosis and DNA replication simulations to look at overall cell effects. 相似文献
82.
Ahmad B Khan H Bashir S Ali M 《Journal of enzyme inhibition and medicinal chemistry》2006,21(6):765-769
The methanolic extract of the corms of Colchicum luteum Baker (Liliaceae) and its subsequent fractions in different solvent systems were screened for antibacterial and antifungal activities. The crude extract and all the fractions demonstrated moderate to excellent antifungal activities against tested pathogens in antifungal bioassay. Excellent antifungal activity was shown against trichophyton longifusus, up to 75%, and microsporum canis, up to 85%, while the crude extract and subsequent fractions showed mild to moderate activities in an antibacterial bioassay with maximum antibacterial activity 58% against Bacillus subtilis. 相似文献
83.
84.
Nadeem Hashmi M. Masroor A. Khan Moinuddin Mohd Idrees Tariq Aftab 《Plant Growth Regulation》2012,68(2):281-291
Fennel (Foeniculum vulgare Mill) is a high-value medicinal and essential oil bearing plant used extensively in pharmaceutical, food and cosmetic industries. A pot experiment was carried out in the natural conditions of net house to resolve whether the foliar application of salicylic acid (SA) might enhance the growth, yield and essential oil production of fennel. Plants were sprayed three times with SA. The first spray was carried out at 40?days after sowing (DAS); the second and third sprays were applied one and 2?weeks later, the plants were sprayed with deionised water (control) and different concentrations of SA (10?5, 10?4 and 10?3?M). The foliar spray of SA at 10?4?M significantly enhanced the vegetative growth (shoot and root lengths, fresh and dry weights), physiological and biochemical characteristics (chl ??a??, chl ??b??, total chlorophyll and carotenoids contents, nitrate reductase activity, carbonic anhydrase activity, leaf-N, -P and -K contents), yield characteristics (number of umbels and fruits, 1,000-seed weight and seed yield) and essential oil yield of fennel. GLC analysis revealed the significant increase in the components of essential oil, viz. trans-anethole (80.4?C84.7?%), methyl chavicol (2.3?C2.5?%) and fenchone (5.6?C7.9?%). It was concluded that foliar spray of SA at 10?4?M might be employed for enhancing the plant growth as well as yield and quality of essential oil of fennel. 相似文献
85.
M. Naeem Mohd. IdreesTariq Aftab M. Masroor A. KhanMoinuddin Lalit Varshney 《Carbohydrate polymers》2012,87(2):1211-1218
Irradiated carrageenan (IC) could elicit plant growth promoting activities in plants. The effect of foliar spray of five concentrations of IC (20, 40, 60, 80 and 100 mg L−1) was studied on Mentha arvensis L. in terms of plant growth, physiological attributes, herbage yield and the content and yield of essential oil and its components. Un-irradiated carrageenan and deionized water had no effect on the attributes studied. GPC study revealed formation of low molecular weight fractions in irradiated samples containing less than 20,000 molecular weight oligomers which are responsible for plant growth promotion in this study. 80 mg L−1 of IC was the most effective concentration which resulted in the highest values of growth attributes, herbage yield and the content and yield of essential oil and menthol content of the oil. It also improved the leaf-nutrient contents, photosynthetic rate and other physiological parameters. 100 mg L−1 of IC did not further improve the attributes studied, but it was always better than the control. 相似文献
86.
Multiple different approaches are being used to activate the immune system against breast cancer. Vaccine therapy in general
follows the principle that injections of various substances ultimately result in the presentation of tumor peptides to the
patient’s immune system. We proposed a potential in silico DNA vaccine against breast cancer by integrating high affinity
T cell (MHC-I and MHC-II) and B cell (continuous and discontinuous) epitopes. The matching of the HLA haplotype and antigen
was performed to provide the appropriate peptide epitope suitable for majority of the patients. The immunogenic nature of
the antigenic construct was also enhanced by the administration of consensus epitopes. The potency of DNA vaccines depends
on the efficient expression and presentation of the encoded antigen of interest and the chances of efficient expression of
our antigenic construct in host organism was also verified by in silico approaches. An attempt was made to overcome the limited
potency of the DNA vaccine by targeting DNA to professional antigen-presenting cells (APCs). A higher immune response theoretically
corresponds to a higher survival rate of patients. Therefore, optimization studies were also employed to enhance the immunogenicity
of proposed in silico DNA vaccine. 相似文献
87.
MH Kim AL Tsuhako EW Co DT Aftab F Bentzien J Chen W Cheng S Engst L Goon RR Klein DT Le M Mac JJ Parks F Qian M Rodriquez TJ Stout JH Till KA Won X Wu FM Yakes P Yu W Zhang Y Zhao P Lamb JM Nuss W Xu 《Bioorganic & medicinal chemistry letters》2012,22(15):4979-4985
Variously substituted indolin-2-ones were synthesized and evaluated for activity against KDR, Flt-1, FGFR-1 and PDGFR. Extension at the 5-position of the oxindole ring with ethyl piperidine (compound 7i) proved to be the most beneficial for attaining both biochemical and cellular potencies. Further optimization of 7i to balance biochemical and cellular potencies with favorable ADME/ PK properties led to the identification of 8h, a compound with a clean CYP profile, acceptable pharmacokinetic and toxicity profiles, and robust efficacy in multiple xenograft tumor models. 相似文献
88.
89.
Background
Nanoparticles (NPs) can potentially cause adverse effects on organ, tissue, cellular, subcellular and protein levels due to their unusual physicochemical properties. Advances in nanotechnology have identified promising candidates for many biological and biomedical applications. Since the properties of NPs differ from that of their bulk materials, they are being increasingly exploited for medical uses and other industrial applications. The aim of the present study was to investigate the particle-size effect of gold nanoparticles (GNPs) on the hepatic tissue in an attempt to cover and understand the toxicity and the potential threat of their therapeutic and diagnostic use. 相似文献90.
U Bashir Aamir N Badar MR Mehmood N Nisar RM Suleman S Shaukat S Sharif J Kamran SS Zaidi BM Kazi L Gubareva X Xu R Garten A Klimov 《PloS one》2012,7(8):e41866