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51.
New Ni(II), Pd(II) and Pt(II) complexes coordinated to azo pyrazolone ligand with a potent anti‐tumor activity: Synthesis,characterization, DFT and DNA cleavage studies
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Eman A. Bakr Gad B. Al‐Hefnawy Mohamed K. Awad Hossam H. Abd‐Elatty Mohamed S. Youssef 《应用有机金属化学》2018,32(2)
The absolute necessity to fight some class of tumor is perceived as serious health concerns, so the discovery and development of effective anticancer agents are urgently needed. (E)‐4‐((2‐hydroxyphenyl)diazenyl)‐3‐phenyl‐1H‐pyrazol‐5(4H)‐one, HL, and its Ni(II), Pd(II) and Pt(II) complexes were synthesized and the biological activity was evaluated for antitumor, antioxidant and antimicrobial activity as well as DNA cleavage. Their structures were assigned depending on the elemental analysis, conductivity, magnetic moment, spectral measurements (IR, 1HNMR, mass and UV–Vis) and thermal analysis. 3D molecular modeling using DFT method confirmed that the geometrical structures agree well with the suggested experimental ones. The antitumor activity was evaluated against four different cell lines using MTT assay. The ligand HL showed a potent cytotoxic activity compared to 5‐fluorouracil as a reference drug. For metal complexes, the order of activity was: Pd(II) > Ni(II) > Pt(II). A remarkable antioxidant activity for the ligand HL was recorded. It was higher than that of the metal complexes. Results of antimicrobial experiments revealed that all compounds were moderate to highly active against selected bacterial strains but inactive as antifungal except Pd(II) which showed a moderate antifungal activity. Gel electrophoresis showed insignificant nucleases activity for the ligand or its metal complexes even in the presence of H2O2 providing protection of DNA from damage. The antitumor activity of our compounds may be not due to DNA cleavage but may be referred to a mechanism similar to that of 5‐fluorouracil which interfere with DNA replication. The present work suggests the use of this ligand in the design and development of new anticancer drugs. 相似文献
52.
Divya Ganesan Eman Al-Sayed Abhishek Albert Eldho Paul Abdel Nasser B. Singab 《Natural product research》2018,32(11):1274-1280
Phytochemicals serve as potential therapeutic agents for the prevention and treatment of diseases. In this study, we elucidate the renoprotective activity of compounds isolated from Eucalyptus globulus and Melaleuca styphelioides extracts in glucose- and oxalate-challenged NRK-49F cell model. The antioxidant potential of isolated compounds was evaluated based on their effect on antioxidant enzyme activities and lipid peroxidation levels. The results demonstrated that exposure of NRK-49F cells to glucose and oxalate stress augmented cell damage and attenuated antioxidant enzyme activities. The phytochemicals 2,2,8-trimethyl-6-formyl-chrom-3-ene-7-O-β-D-glucopyranoside, Cornusiin B and tellimagrandin I treatment restored antioxidant enzyme activity, significantly lowered lipid peroxidation levels and effectively protected cells from glucose and oxalate stress equivalent to the known antioxidant, N-acetyl cysteine. Pterocarinin A significantly reversed cellular damage owing to glucose stress. In conclusion, the compounds isolated from E. globulus and M. styphelioides showed potential cytoprotective and anti-oxidative property against glucose- and oxalate-induced oxidative stress in NRK-49F cells. 相似文献
53.
L. V. Batog V. Yu. Rozhkov L. S. Konstantinova V. E. Eman M. O. Dekaprilevich Yu. T. Struchkov S. E. Semenov O. V. Lebedev L. I. Khmel'nitskii 《Russian Chemical Bulletin》1996,45(5):1189-1193
The oxidative cyclocondensation of 3,4-diaminofurazan and 4,4-diamino-3,3-azofurazan with dibromoisocyanurate afforded macrocyclec polydiazenofurazans. The reaction can be directed towards the formation of both the four-membered cycle alone or the three-, six-, and eight-membered macrocycles.Translated fromIzvestiya Akademii Nauk. Seriya Khimicheskaya, No. 5, pp. 1250–1254, May, 1996.Deceased in 1995. 相似文献
54.
Bertelli M El-Bastawissy E Knaggs MH Barrett MP Hanau S Gilbert IH 《Journal of computer-aided molecular design》2001,15(5):465-475
A number of triphenylmethane derivatives have been screened against 6-phosphogluconate dehydrogenase from Trypanosoma brucei and sheep liver. Some of these compounds show good inhibition of the enzymes and also selectivity towards the parasite enzyme. Modelling was undertaken to dock the compounds into the active sites of both enzymes. Using a combination of DOCK 3.5 and FLEXIDOCK a correlation was obtained between docking score and both activity for the enzymes and selectivity. Visualisation of the docked structures of the inhibitors in the active sites of the enzymes yielded a possible explanation of the selectivity for the parasite enzyme. 相似文献
55.
Adel A.-H. Abdel-Rahman Ahmed E.-S. Abdel-Megied Mohamed A. M. Hawata Eman R. Kasem Mohamed T. Shabaan 《Monatshefte für Chemie / Chemical Monthly》2007,16(6):889-897
Chalcones were synthesized by a base catalyzed Claisen-Schmidt condensation reaction. Bromination of chalcones afforded the dibromo derivatives. Monobromo derivatives could be obtained
by treating the corresponding dibromochalcones with dry benzene in the presence of triethylamine. Pyrazole derivatives were
obtained by refluxing of dibromochalcones with phenylhydrazine or 2,4-dinitrophenylhydrazine in dry pyridine. Chalcones were
treated with hydrazine hydrate or phenyl hydrazine in ethanol to afford Δ
2-pyrazolines and N-phenyl-Δ
2-pyrazolines. Condensation of chalcones with hydroxylamine hydrochloride or thiourea in ethanolic sodium hydroxide solution
gave 4,5-dihydroisoxazoles and 5,6-dihydropyrimidine-2-(1H)-thiones. The prepared compounds were tested for antimicrobial activity against four different bacterial species displaying
different degrees of antibacterial activities or inhibitory actions. 相似文献
56.
Jan C. van Dam Michael R. Eman Johannes Frank Hans C. Lange Gijs W. K. van Dedem Sef J. Heijnen 《Analytica chimica acta》2002,460(2):307-218
The purpose of this study is to selectively and quantitatively analyze several glycolytic intermediates in cells of Saccharomyces cerevisiae using high-performance anion exchange chromatography (HPAEC) coupled to electrospray ionization tandem mass spectrometry for the analysis. A sodium hydroxide gradient is used to separate the glycolytic compounds and after the column sodium hydroxide is reduced by proton exchange with a membrane device prior to introduction to the mass spectrometer. The detection limits for 10 μl samples are down to the 0.4–5 pmol range. This corresponds for the intracellular metabolites to a range of 2–20 nmol per gram biomass dry weight (DW). Standard addition did reveal some influence of the sample matrix on the measured concentrations. Separation and analysis is hardly affected by the high sulfate and phosphate concentrations (1 mM) in the fermentation medium and by the intracellular matrix. Validation of the glucose-6-phosphosphate LC–MS–MS analysis results with enzymatic analysis showed an excellent agreement between the two methods. The suitability of the method was clearly shown by analyzing a series of steady state S. cerevisiae samples from a carbon limited aerobic chemostat culture. 相似文献
57.
Ahmed A. Abdel-Khalek El-Said M. Sayyah Eman S. H. Khalid 《Transition Metal Chemistry》1993,18(6):555-558
Summary The kinetics of oxidation of [CoII(EDTA)]2- (EDTA = ethylenediaminetetraacetate) by N-bromosuccinimide (NBS) in aqueous solution obey the equation: Rate = k
2
K
3[CoII]T[NBS]/{1 + [H+]/K
2 + K
3[NBS]} where k
2 is the rate constant for the electron-transfer process, K
2 the equilibrium constant for the dissociation of [CoII(EDTAH)(H2O)]– to [CoII(EDTA)(OH)]3– and K
3 the pre-equilibrium formation constant. The activation parameters are reported. It is proposed that electron transfer proceeds via an inner-sphere mechanism with the formation of an intermediate which slowly generates hexadentate[CoIII(EDTA)]–.Abstracted from the M.Sc. thesis of Eman S. H. Khaled. 相似文献
58.
Preparation of fluorescein isothiocyanate (FITC)-encapsulated silica nanoparticles (F-SiNPs) via seven different approaches to be used as developing agents for fingerprints detection is presented in this report. In this study, the suitability of each synthesis route toward incorporation of the selected fluorophore into silica matrix and its efficiency in fingerprints detection were systematically studied. The composition of the particles was designed to examine the hydrophobic and dipole-dipole interactions between the silicate backbone and both of the fluorescent reporter molecules and the fingerprint residues. F-SiNPs were prepared with two conventional sol-gel approaches; the Stöber method and the water in oil reverse microemulsion (WORM) method. The alkoxysilane precursor, tetraethoxyorthosilicate (TEOS) and its binary mixtures with phenyltriethoxysilane (PTEOS) or 3-aminopropyl triethoxysilane (APTES) have been used in preparing the F-SiNPs to study the effect of nanoparticles composition on fingerprints development. In addition, FITC was conjugated with APTES so it can be covalently bonded to the silica matrix and to be compared with non-covalently FITC-doped SiNPs. Moreover, the enhancement effect of introducing polyvinylpyrrolidone (PVP) onto the surface of the less hydrophobic F-SiNP on fingerprints detection on different non-porous surfaces was also investigated. The mean diameters of the F-SiNPs were between 4.1?±?0.6 and 110.4?±?31.1 nm as obtained from the TEM size measurement for the nanoparticles prepared by the WORM and Stöber methods, respectively. The obtained results clearly highlight the advantages of using a mixture of TEOS and PTEOS alkoxysilane precursors in preparing F-SiNPs with remarkable encapsulation efficiency and clear detection of fingerprints due to efficient embedding of the fluorophore inside the silica network even without conjugation. It was also observed that both the Stöber and WORM methods can be used in preparing the F-SiNPs developing agents and that PVP coated particles did not show any significant enhancement in fingerprints visualization. 相似文献
59.
Seven tetrazole-thione complexes, [Pd2(κ2-ptt)4]( 1 ), trans-[Pd(k1-S-ptt)2(PPh3)2] ( 2 ), trans-[Pd(k1-S-ptt)2(SPPh3)2] ( 3 ), trans-[Pd(k1-S-ptt)2(OPPh3)2] ( 4 ), [Pd(k1-N-ptt)2(k2-dppe)] ( 5a ), [Pd(k1-S-ptt)2(k2-dppe)] ( 5b ), [Pd(k1-S-ptt)2(k2-dppeS2)] ( 6 ), and [Pd(k1-S-ptt)2(k2-dppeO2)] ( 7 ), were prepared from 1-phenyl-1H-tetrazole-5-thiol (Hptt), with substituted phosphines. These complexes were investigated by CHNS analysis; infrared (IR), nuclear magnetic resonance (NMR) (1H and 31P), and ultraviolet–visible (UV–Vis) spectroscopy; and single-crystal X-ray data for 5b . In Complex 1 , the ptt− ligand adopted μ2- k-N, k-S bridging mode to afford a dimeric complex, whereas in Complexes 2–4 , 6 , and 7 , the ptt− was covalently coordinated via sulfur atom of the thiol group as a solo product. In contrast, in Complex 5 , the ptt− ligand was bonded in a monodentate fashion through a deprotonated tetrazole ring nitrogen atom in isomer 5a or via a thiolato sulfur atom in isomer 5b . These linkage isomers were clearly shown in the 31P-{1H} NMR. To explain the adoption of the ligand binding modes in Complexes 5a and 5b , geometry optimization calculations were carried out on two isomers. Very small differences of all molecular parameters were found between 5a and 5b isomers. This confirms the reason for obtaining two isomers. Also, theoretical studies are made for all compounds, and excellent agreement is obtained with experimental data. The direct band gap (Eg) values are equal to 2.88, 2.85, and 2.45 eV for Complexes 1 , 2 , and 4 , respectively, revealing a semiconductor nature. The inhibition activity of Complexes 1–3 , 5 , and 8 were evaluated versus the growth of four types of bacteria in vitro. The complexes showed a good activity compared with free ligand and a standard antibiotic. 相似文献
60.
A new series of metal complexes containing Co(II), Pd(II), Fe(III) chloride and Cu(II) salts (chloride, bromide, sulphate and perchlorate) have been prepared with Schiff base ligand ( HL ). The synthesized compounds were elucidated using elemental analyses, spectral techniques, molar conductance, magnetic measurements and thermogravimetric studies. The analytical data established (1 M:1 L) stoichiometry for complexes ( 1 ), ( 2 ), ( 4 ), ( 6 ) and ( 7 ) as well as (1 M:2 L) and (2 M:3 L) stoichiometry for complexes ( 5 ) and ( 3 ), respectively. As a result, the ligand HL coordinates in complexes ( 1 ), ( 2 ), ( 4 ), ( 6 ) as a monobasic tridentate ONN moiety via the oxygen atom of the deprotonated phenolic OH, the nitrogen atoms of the azomethine and the imine group in pyrazolopyridine ring. While, it behaves as a neutral bidentate in complexes ( 3 , 7 ), chelates via oxygen and nitrogen atoms of enolic OH and azomethine groups. Also, in complex ( 5 ) Cu2+ ion binds via NO sits of two ligand molecules in its monobasic and neutral forms. The magnetic moment and electronic spectral data proposed octahedral structure for complexes ( 2 , 3 and 7 ) as well as triagonal bipyramidal and square pyramidal geometry for complexes ( 1 and 4 ), while, chelates ( 5 ) and ( 6 ) possess square planar geometry. TG/DTG studies confirmed the chemical formula for these complexes and established the thermal decomposition processes ended with the formation of metal or metal oxides contaminated with carbon residue. An axial electron spin resonance spectra were suggested for Cu(II) complexes pointing to 2B1g as a ground state with hyperfine structure for complex ( 4 ). In vitro antibacterial and antioxidant activities were performed for HL ligand and its metal complexes. The biological studies indicate that complex ( 3 ) has better antibacterial activity compared to the ligand and the other complexes. 相似文献