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961.
以靛红酸酐为起始原料,经硝化、还原上保护、氨解开环、环合、卤素交换和脱保护共七步反应合成了氟喹酮(7),其结构经 1H NMR,13C NMR和ESI-MS确证。研究了硝化试剂、溶剂、催化剂等对7收率的影响,结果表明:在使用浓硝酸作为硝化试剂,甲苯,乙腈等为溶剂,Raney-Ni, TBAB等为催化剂时,总收率可达58%,纯度达99%以上。 相似文献
962.
光敏感的纳米载体因其可从时间和空间上精确地控制药物的释放以实现对肿瘤的高效治疗,近年来逐渐成为生物医学领域的研究热点之一。本文综述了光敏感的纳米载体破裂从而释放出装载的药物的三种机理,主要包括:(1)光致异构化引发的纳米载体形态转变;(2)光反应引发的纳米载体降解;(3)光热引发的纳米载体破裂。本文简单介绍了这三种释放机理,例举了这三种释放机理所对应的光敏感材料,并阐述了其在药物运输、可控释放以及肿瘤治疗中的最新研究进展以及存在的问题,为光敏感纳米载体在生物体系中的应用提供参考,并对今后的发展作了展望。 相似文献
963.
964.
Chanon Suyamud Chanita Phetdee Thanapak Jaimalai Panchika Prangkio 《Molecules (Basel, Switzerland)》2021,26(16)
Despite much progress in cancer therapy, conventional chemotherapy can cause poor biodistribution and adverse side-effects on healthy cells. Currently, various strategies are being developed for an effective chemotherapy delivery system. Silk fibroin (SF) is a natural protein used in a wide range of biomedical applications including cancer therapy due to its biocompatibility, biodegradability, and unique mechanical properties. In this study, SF-coated liposomes (SF-LPs) were prepared as a biomimetic drug carrier. Physicochemical properties of SF-LPs were characterized by Fourier-transform infrared spectroscopy (FTIR), dynamic light scattering, zeta potential measurement, and transmission electron microscopy (TEM). In vitro release of SF-LPs loaded with doxorubicin (DOX-SF-LPs) was evaluated over 21 days. Anticancer activity of DOX-SF-LPs was determined against MCF-7 and MDA-MB231 cells using the MTT assay. SF-LPs containing 1% SF exhibited favorable characteristics as a drug carrier. SF coating modified the kinetics of drug release and reduced the cytotoxic effect against L929 fibroblasts as compared to the uncoated liposomes containing cationic lipid. DOX-SF-LPs showed anticancer activity against breast cancer cells after 48 h or 72 h at 20 μM of DOX. This approach provides a potential platform of long-term release that combines biocompatible SF and phospholipids for cancer therapy, achieving efficient drug delivery and reducing side-effects. 相似文献
965.
Cindy B. McReynolds Jun Yang Alonso Guedes Christophe Morisseau Roberto Garcia Heather Knych Caitlin Tearney Briana Hamamoto Sung Hee Hwang Karen Wagner Bruce D. Hammock 《Molecules (Basel, Switzerland)》2021,26(16)
There are few novel therapeutic options available for companion animals, and medications rely heavily on repurposed drugs developed for other species. Considering the diversity of species and breeds in companion animal medicine, comprehensive PK exposures in the companion animal patient is often lacking. The purpose of this paper was to assess the pharmacokinetics after oral and intravenous dosing in domesticated animal species (dogs, cats, and horses) of a novel soluble epoxide hydrolase inhibitor, EC1728, being developed for the treatment of pain in animals. Results: Intravenous and oral administration revealed that bioavailability was similar for dogs, and horses (42 and 50% F) but lower in mice and cats (34 and 8%, respectively). Additionally, clearance was similar between cats and mice, but >2× faster in cats vs. dogs and horses. Efficacy with EC1728 has been demonstrated in mice, dogs, and horses, and despite the rapid clearance of EC1728 in cats, analgesic efficacy was demonstrated in an acute pain model after intravenous but not oral dosing. Conclusion: These results demonstrate that exposures across species can vary, and investigation of therapeutic exposures in target species is needed to provide adequate care that addresses efficacy and avoids toxicity. 相似文献
966.
967.
Ewa Oledzka Marcelina Dyrka Marcin Sobczak Anna Zgadzaj Grzegorz Nalecz-Jawecki 《高分子科学杂志,A辑:纯化学与应用化学》2016,53(3):169-176
This paper describes the development of covalent star-shaped poly(L-lactide/?-caprolactone) random copolymer-oxprenolol (OXP) conjugates as a potential approach to controlling drug release from implantable delivery systems. We prepared synthesized materials containing 14–17 mol% OXP, which were conjugated via an ester bond. The conjugates, which were composed of biodegradable copolyester chains, natural genistein as a central core and drug, were characterized by hydrogen nuclear magnetic resonance (1H-NMR), Fourier transform infrared spectroscopy (FTIR) and viscosity methods. We evaluated the cyto- and genotoxicity of the synthesized copolymeric matrices, followed by the conjugates, with bacterial luminescence, protozoan and Salmonella typhimurium TA1535 assays. Furthermore, we performed in vitro mammalian assays of the obtained products with V79 cells. We found that the in vitro release of OXP from the obtained star-shaped conjugates was dependent on the structure of the synthesized biodegradable matrices. 相似文献
968.
以溶剂热法制备氨基功能化的Fe_3O_4纳米颗粒为磁核,结合溶胶-凝胶法和模板法在其表面先后包覆上致密的SiO_2层和介孔TiO_2层,制备了磁性-发光-微波热转换性-介孔结构为一体的多功能核-壳结构纳米复合颗粒,并对其结构、性能及载药能力进行了研究。XRD分析表明:Fe_3O_4表面包覆上了无定形结构的SiO_2和TiO_2。TEM照片表明:所得的纳米复合颗粒具有明显的核壳结构和完美的球形,构成核的Fe_3O_4颗粒的尺寸在40~50 nm之间,Fe_3O_4@SiO_2@mTiO_2核壳结构纳米复合颗粒的尺寸为60~70 nm,壳层厚度约10 nm,并可观察到壳层中清晰的孔状结构。磁性、荧光光谱和微波热转换特性分析表明:该复合颗粒同时具有良好的发光性、磁性和微波热转换特性。N_2气吸附及药物负载率分析表明,该复合颗粒具有较高的比表面积(640 m~2·g~(-1))和介孔结构(孔径约2.8 nm)并且具有较高的药物负载率。 相似文献
969.
建立了高效液相色谱-串联质谱(HPLC-MS/MS)同时测定生猪尿液中喹诺酮类、磺胺类、磺胺增效剂、四环素类、林可胺类、大环内脂共29种限用兽药残留量的检测方法。试样经乙酸铵和EDTA-Na缓冲液提取,HLB固相萃取小柱净化后,HPLC-MS/MS进行测定,其中β-受体激动剂类用内标法定量,其余兽药用外标法定量。在电喷雾电离正离子模式下,以多反应监测(MRM)方式采集数据进行定性与定量分析。29种兽药在猪尿基质中标准曲线的线性系数(r)均大于0.99,3个不同加标水平下的平均回收率为58%~108%,日内相对标准偏差(RSD)为1.9%~18.9%,日间RSD为3.4%~20.9%;定量下限(LOQ,S/N≥10)为1.0~10.0μg/L。该方法经济、高效、可靠,可用于生猪屠宰前兽药多残留的快速检测。 相似文献
970.
Transformable Peptide Nanocarriers for Expeditious Drug Release and Effective Cancer Therapy via Cancer‐Associated Fibroblast Activation
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Tianjiao Ji Dr. Ying Zhao Dr. Yanping Ding Jing Wang Ruifang Zhao Jiayan Lang Hao Qin Xiaoman Liu Jian Shi Dr. Ning Tao Prof. Dr. Zhihai Qin Prof. Dr. Guangjun Nie Prof. Dr. Yuliang Zhao 《Angewandte Chemie (International ed. in English)》2016,55(3):1050-1055
A novel cleavable amphiphilic peptide (CAP) was designed to be specifically responsive to fibroblast activation protein‐α (FAP‐α), a protease specifically expressed on the surface of cancer‐associated fibroblasts. The CAP self‐assembled into fiber‐like nanostructures in solution, while the presence of hydrophobic chemotherapeutic drugs readily transformed the assemblies into drug‐loaded spherical nanoparticles. The disassembly of these nanoparticles (CAP‐NPs) upon FAP‐α cleavage resulted in rapid and efficient release of the encapsulated drugs specifically at tumor sites. This Transformers‐like drug delivery strategy could allow them to disrupt the stromal barrier and enhance local drug accumulation. Therapeutic results suggested that drug‐loaded CAP‐NPs hold promising tumor specificity and therapeutic efficacy for various solid tumor models, confirming its potential utility and versatility in antitumor therapy. 相似文献