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81.
Dioxins invade the body mainly through the diet, and produce toxicity through the transformation of aryl hydrocarbon receptor (AhR). An inhibitor of the transformation should therefore protect against the toxicity and ideally be part of the diet. We examined flavonoids ubiquitously expressed in plant foods as one of the best candidates, and found that the subclasses flavones and flavonols suppressed antagonistically the transformation of AhR induced by 1 nM of 2,3,7,8-tetrachlorodibenzo-p-dioxin, without exhibiting agonistic effects that transform AhR. The antagonistic IC(50) values ranged from 0.14 to 10 microM, close to the physiological levels in human. 相似文献
82.
New Hydrazides and Hydrazide‐Hydrazones of 2,3‐Dihalogen Substituted Propionic Acids: Synthesis and in vitro Antimicrobial Activity Evaluation 下载免费PDF全文
The main aim of this research was the synthesis, spectral identification and in vitro antimicrobial evaluation of new hydrazides and hydrazide‐hydrazones of 2,3‐dihalogen substituted propionic acids. New hydrazides were obtained by the substitution reaction of appropriate ethyl esters of 2,3‐dihalogen substituted propionic acids with hydrazine hydrate. Then obtained hydrazides were subjected to condensation reaction with various aldehydes which yielded with new hydrazide‐hydrazone derivatives. All obtained compounds were identified on the basis of spectral methods (1H‐NMR, 13C‐NMR) and in vitro screened against a panel of bacterial and fungal strains according to EUCAST and CLSI guidelines. 相似文献
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Elżbieta Galoch Joanna Czaplewska Elżbieta Burkacka-Łaukajtys Jan Kopcewicz 《Plant Growth Regulation》2002,37(3):199-205
The influence of BA, GA3 and IAA applied successively onflower bud formation in shoot apices of Pharbitis nil hasbeen investigated. The shoot apices were isolated from seedlings cultivatedunder non-inductive continuous light and from seedlings exposed to asubinductive (12 h) dark period. BA and GA3 introducedsuccessively into culture medium replaced the inductive night, causing theflowering of plantlets in completely non-inductive continuous light (optimalconcentration of BA – 10–7–10–6mol dm–3, GA3 –10–7–10–6 moldm–3) and stimulated this process under thesubthresholdinduction. These hormones applied in reverse sequence (in the first placeGA3, then BA) did not affect flowering of explants. IAA nullifiedthestimulating effect of BA and GA3. The influence of phytohormones onflowering may result from the change of growth correlations within the shootapical meristem. 相似文献
86.
Minarowska A Gacko M Karwowska A Minarowski Ł 《Folia histochemica et cytobiologica / Polish Academy of Sciences, Polish Histochemical and Cytochemical Society》2008,46(1):23-38
A literature survey was performed of human cathepsin D gene, cathepsin D biosynthesis, posttranslatory modifications, transport within the cell, substrate specificity and catalytic effect. Methods used to determine the activity and level of this proteinase as well as its role in the biochemistry and pathobiochemistry of cells, tissues and organs were considered. 相似文献
87.
Salvadori S Fiorini S Trapella C Porreca F Davis P Sasaki Y Ambo A Marczak ED Lazarus LH Balboni G 《Bioorganic & medicinal chemistry》2008,16(6):3032-3038
H-Dmt-Tic-NH-CH(2)-Bid (UFP-502) was the first delta-opioid agonist prepared from the Dmt-Tic pharmacophore. It showed interesting pharmacological properties, such as stimulation of mRNA BDNF expression and antidepression. To evaluate the importance of 1H-benzimidazol-2-yl (Bid) in the induction of delta-agonism, it was substituted by similar heterocycles: The substitution of NH(1) by O or S transforms the reference delta-agonist into delta-antagonists. Phenyl ring of benzimidazole is not important for delta-agonism; in fact 1H-imidazole-2-yl retains delta-agonist activity. 相似文献
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Łukasz Jaremko Mariusz Jaremko Paweł Pasikowski Marek Cebrat Piotr Stefanowicz Marek Lisowski Jolanta Artym Michał Zimecki Igor Zhukov Zbigniew Szewczuk 《Biopolymers》2009,91(6):423-431
Recently, ubiquitin was suggested as a promising anti‐inflammatory protein therapeutic. We found that a peptide fragment corresponding to the ubiquitin50–59 sequence (LEDGRTLSDY) possessed the immunosuppressive activity comparable with that of ubiquitin. CD and NMR spectroscopies were used to determine the conformational preferences of LEDGRTLSDY in solution. The peptide mixture, obtained by pepsin digestion of ubiquitin, was even more potent than the intact protein. Although the peptide exhibited a well‐defined conformation in methanol, its structure was distinct from the corresponding 50–59 fragment in the native ubiquitin molecule. © 2009 Wiley Periodicals, Inc. Biopolymers 91: 423–431, 2009. This article was originally published online as an accepted preprint. The “Published Online” date corresponds to the preprint version. You can request a copy of the preprint by emailing the Biopolymers editorial office at biopolymers@wiley.com 相似文献