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31.
PEPAMP是应用于工业循环水中的新一代高效阻垢剂.采用电喷雾电离质谱和质谱/质谱技术分析了合成产物,注射泵直接进样,正离子方式检测,方法简便、快速.通过EI-MS技术获得了目标产物PEPAMP及主要副产物的准分子离子峰,通过ESI-MS-MS技术获得了其碎片信息,并对目标化合物及主要副产物进行了精确质量测定,确定了目标化合物及主要副产物的结构. 相似文献
32.
Chao Zhang 《Tetrahedron》2007,63(26):5832-5838
The ability to inhibit any protein kinase of interest with a small molecule is enabled by a combination of genetics and chemistry. Genetics is used to modify the active site of a single kinase to render it distinct from all naturally occurring kinases. Next, organic synthesis is used to develop a small molecule, which does not bind to wild-type kinases but is a potent inhibitor of the engineered kinase. This approach, termed chemical genetics, has been used to generate highly potent mutant kinase-specific inhibitors based on a pyrazolopyrimidine scaffold. Here, we asked if the selectivity of the resulting pyrazolopyrimidines could be improved, as they inhibit several wild-type kinases with low-micromolar IC50 values. Our approach to improve the selectivity of allele-specific inhibitors was to explore a second kinase inhibitor scaffold. A series of 6,9-disubstituted purines was designed, synthesized, and evaluated for inhibitory activity against several kinases in vitro and in vivo. Several purines proved to be potent inhibitors against the analog-sensitive kinases and exhibited greater selectivity than the existing pyrazolopyrimidines. 相似文献
33.
Wolfgang Benetka Manfred Koranda Frank Eisenhaber 《Monatshefte für Chemie / Chemical Monthly》2006,137(10):1241-1281
Summary. Since 1979, when prenylation has been first discovered as chemical oddity of a yeast mating factor, the two forms of this
posttranslational modification of proteins (farnesylation and geranylgeranylation) have been found as wide spread among proteins
from Eukarya and their viruses. This review attempts to summarize as comprehensively as possible the enzymological processes
of prenylation and the various aspects of their biological significance.
The substrate proteins of prenyltransferases are known to carry a sequence signal composed of a cysteine-containing 4–5 residue
stretch at the utmost C-terminal end that is N-terminally preceded by a flexible and polar linker region of ca. 10 residues. Postprenylation processing of substrate proteins can involve C-terminal proteolysis, C-terminal carboxyl methylation,
and other steps of maturation. The prenyl anchor functions as module for membrane attachment or for protein–protein interaction.
Prenyl anchor carrying proteins fulfill a large array of functions in signaling and regulation of cellular processes. Therefore,
they are involved in the pathogenesis of a variety of human diseases, the most prominent one being cancer. Farnesyltransferase
inhibitors show surprisingly high efficiency in controlling tumor growth in model systems but, so far, clinical trials with
human patients have remained without the desired success. Interference into prenylation pathways appears also a promising
treatment principle in a variety of parasitic diseases. 相似文献
34.
35.
Toshio Morikawa Osama Bashir Abdel-Halim Hisashi Matsuda Osamu Muraoka Masayuki Yoshikawa 《Tetrahedron》2006,62(26):6435-6442
Three new pseudoguaiane-type sesquiterpenes, dichrocepholides A-C, and two new pseudoguaiane-type sesquiterpene dimers, dichrocepholides D and E, were isolated from the aerial part of Dichrocephala integrifolia. Their stereostructures were determined on the basis of chemical and physicochemical evidence. In addition, the extract and its principal sesquiterpene constituent, parthenin, showed an inhibitory activity on nitric oxide (NO) production and on induction of inducible NO synthase. 相似文献
36.
LIN Jun ** MAO De-shou XU Rong YAN Sheng-jiao YANG Li-juan LI Jun-feng LIU Fu-chu . Department of Applied Chemistry Yunnan University Kunming P. R. China . The Dyson Perrins Laboratory University of Oxford South Parks Road Oxford OX QY UK 《高等学校化学研究》2004,(4)
IntroductionThe insecticidal activity of benzoylphenylurea( BPU ) analogues,discovered in the early1 970′s[1_ 4] ,is connected with the process ofmoult-ing and appears to affect the chitin synthesis of in-sects. The benzoylphenylurea class of insectgrowth regulators( IGRs) ,interfere with chitinsynthesis in target pests,causing death or abortivedevelopment and are considered to be the fourthgeneration of insecticides or novel materials for in-sect control.Benzoylphenylurea type insecticides… 相似文献
37.
碳五馏分中微量阻聚剂二乙基羟胺的气相色谱测定法 总被引:2,自引:0,他引:2
提出采用HP-l毛细管色谱柱测定碳五馏分中微量阻聚剂二乙基羟胺组分的气相色谱方法。在本文提出的条件下,二乙基羟胺与其他组分分离良好,检出限低于20mg/kg,相对标准偏差为3.86%,结果准确可靠,方法满足控制分析的要求。 相似文献
38.
QSAR Studies on the COX-2 Inhibition by 3,4-Diarylcycloxazolones Based on MEDV Descriptor 总被引:2,自引:0,他引:2
Selective inhibition of cyclooxygenase-2 (COX-2) might avoid the side effects of current available nonsteroidal antiinflammatory drugs while retaining their therapeutic efficacy. A novel variable selection and modeling method based on prediction is developed to construct the quantitative structure-activity relationships (QSAR) between the molecular electronegativity distance vector (MEDV) based on 13 atomic types and the biological activities of a set of selective cyclooxygenase-2 inhibitory molecules, 3,4-diarylcycloxazolones (DAA) plus indomethacin,naproxen, and celecoxib. Using multiple linear regression, a 5-variable linear model is developed with the calibrated correlation coefficient of 0.9271 and root mean square error of 0.17 in modeling stage and the validated correlation coefficient of 0.9030 and root mean square error of 0.20 in leave-one-out validation step, respectively. To further test the predictive ability of the model, 20 DAA compounds are picked up to construct a training set which is used to build a QSAR model and then the model is employed to predict the biological activities of the balance compounds. The predicted correlation coefficient and root mean square error are 0.9332 and 0.19, respectively. 相似文献
39.
IntroductionAcetolactatesynthase(ALS)isthefirstcommonenzymeinthebiosyntheticpathwayforthebranched-chainaminoacidsvaline,leucineandisoleucine.Itisaveryeffectivetargetsiteforherbicidalaction,whichistheselectedmodeofactionasitisspecificforplantsanddoesnotaffectmammals.Sulfonylureaherbicidesareanewclassofherbicidesdiscoveredinthemid-l97O'sl.ItsmodeofactionhasbeenestablishedtobeinhibitorytowardALS2.Muchattentionhasbeenfocusedonthiskindofcompounds,sincetheyhaveexcellentactivity,ahighdegreeofseIe… 相似文献
40.
A synthesis and stereochemistry confirmation of a constituent recently isolated from the whole plant Isodon excisus is reported. An enantioselective catalytic boron-mediated reduction of an α-bromoketone was utilized in the key synthetic transformation. The methodology described herein was also used for the synthesis of the natural product's enantiomer and several derivatives. In addition, the compounds were evaluated for inhibitory activity in a caspase induction assay. The natural product was found to be devoid of activity, but several derivatives had moderate inhibitory activity (EC50<1 μM). 相似文献