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111.
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Yuki Hirose Kaori Hashiya Dr. Toshikazu Bando Prof. Dr. Hiroshi Sugiyama 《Chemistry (Weinheim an der Bergstrasse, Germany)》2021,27(8):2782-2788
Hairpin pyrrole-imidazole polyamides (hPIPs) and their chlorambucil (Chb) conjugates (hPIP-Chbs) can alkylate DNA in a sequence-specific manner, and have been studied as anticancer drugs. Here, we conjugated Chb to a cyclic PIP (cPIP), which is known to have a higher binding affinity than the corresponding hPIP, and investigated the DNA alkylation properties of the resulting cPIP-Chb using the optimized capillary electrophoresis method and conventional HPLC product analysis. cPIP-Chb conjugate 3 showed higher alkylation activity at its binding sites than did hPIP-Chb conjugates 1 and 2 . Subsequent HPLC analysis revealed that the alkylation site of conjugate 3 , which was identified by capillary electrophoresis, was reliable and that conjugate 3 alkylates the N3 position of adenine as do hPIP-Chbs. Moreover, conjugate 3 showed higher cytotoxicity against LNCaP prostate cancer cells than did conjugate 1 and cytotoxicity comparable to that of conjugate 2 . These results suggest that cPIP-Chbs could be novel DNA alkylating anticancer drugs. 相似文献
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Lubov' V. Snegur Yury S. Nekrasov Nataliya S. Sergeeva Zhanna V. Zhilina Vera V Gumenyuk Zoya A. Starikova Alexander A. Simenel Nataliya B. Morozova Irina K. Sviridova Valery N. Babin 《应用有机金属化学》2008,22(2):139-147
The toxicity of ferrocenylethyl benzotriazole ( 1 ) and other ferrocene compounds including ferrocenylmethyl benzimidazoles ( 4,5,6,11 ), ferricenium salts ( 3,9,10 ) and ferrocenylmethyl adenine ( 7 ), was studied. All ferrocene complexes under investigation showed low or medium toxicities. On the basis of an earlier model of chemical carcinogenesis, the antitumor activity of ferrocenylalkyl azoles 1, 8 and ferricenium salts 9, 10 was studied in vivo in the so‐called sub‐capsular test on human tumors. This effectiveness was compared with that of cisplatin. A series of ferrocenylalkyl azoles were synthesized by interacting azoles either with α‐hydroxyalkyl ferrocenes FcC(OH)R1R2 in organic solvent in the presence of aqueous HBF4 in quantitative yields or with trimethyl(aminomethyl)ferrocene iodide in an aqueous‐basic medium in good yields. The X‐ray determinations of molecular and crystal structures of α‐(1‐benzotriazolyl)ethylferrocene ( 1 ) and α‐(1‐naphthatriazolyl)ethylferrocene ( 12 ) were performed. Copyright © 2008 John Wiley & Sons, Ltd. 相似文献
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A series of novel tetraphenylantimony derivatives of exo‐7‐oxa‐bicyclo[2,2,1] heptane (ene)‐3‐arylamide‐2‐acid of the general formula Ph4SbO2CCHCHCH2CH2CH(O)HCONHAr (Ar = Ph,4‐ClC6H4, 4‐BrC6H4, 3‐BrC6H4, 4‐F‐3‐ClC6H3 and 4‐MeC6H4) have been synthesized and characterized by elemental analysis, IR, 1H NMR and mass spectra. The crystal structure of Ph4SbO2CCHCHCH2CH2CH(O)HCONHC6H4CH3·CHCl3 was determined by X‐ray diffraction. Five human neoplastic cell lines (HL‐60, KB, Bel‐7402, BGC‐823 and HCT‐8) were used to screen these compounds. The results indicate that these compounds at 10 µM show certain in vitro antitumor activities. Copyright © 2001 John Wiley & Sons, Ltd. 相似文献
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Knoevenagel condensate Schiff base ligands [L = 3‐cinnamalideneacetylacetone‐thiosemicarbazone (CAT)/3‐cinnama‐ lideneacetylacetoneethylthiosemicarbazone (CAET)/3‐cinnamalideneacetylacetonephenylthiosemicarbazone (CAPT)] and their copper/zinc complexes were synthesized. They were characterized by analytical and spectral techniques. From these data it was found that the ligands adopt square‐planar geometry on metalation with Cu2+ and Zn2+. To evaluate the antitumor and cytotoxic activity of the synthesized complexes in mice and human cancer cell lines, the antitumor activity of the complexes was evaluated against an Ehrlich ascites carcinoma (EAC) tumor model. The activity was assessed using survival time and short‐term in vitro cytotoxic activity. Oral administration of complexes (100 mg/kg) increased the survival time. The cytotoxic activity of complexes was evaluated using human breast cancer (MDA‐MB‐231), colon cancer (HCT‐116) and nonsmall lung cancer (NCI‐H‐23) cell lines. Both the complexes possessed significant antitumor and cytotoxic activity on EAC and human cancer cell lines. The in vitro antimicrobial screening effect of the investigated compounds was also tested against the various organisms by well diffusion method. Copyright © 2009 John Wiley & Sons, Ltd. 相似文献
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Dong-Dong Li Xiu-Mei Zhao Na Gu Shuang Zhi Zun-Wei Tao 《Journal of Coordination Chemistry》2017,70(12):2113-2127
Three binuclear phenolate complexes, [Ni2(L1)2(OAc)](BPh4)·DMF (1), [Ni2(L2)2(OAc)](BPh4) (2), and [Ni2(L3)2(OAc)](OH)·3H2O (3), where L1 = 2-{[bis-(2-hydroxy-ethyl)-amino]-methyl}-4-methyl-phenol, L2 = 2-{[bis-(2-hydroxy-ethyl)-amino]-methyl}-4-methoxy-phenol, and L3 = 2-{[bis-(2-hydroxy-ethyl)-amino]-methyl}-4-tert-butyl-phenol), have been synthesized. Single-crystal diffraction reveals that all the metal atoms are in a distorted octahedral geometry. The interactions of the complexes with calf thymus DNA (CT-DNA) have been investigated by UV–vis absorption, fluorescence emission, and circular dichroism spectroscopy and viscosity measurements. Furthermore, DNA cleavage mechanism shows that the complexes may be capable to promote DNA cleavage through oxidative DNA damage pathway, which is indicative of the involvement of hydroxyl radical, singlet oxygen, or singlet oxygen-like entity in the cleavage process. Cytotoxicity studies on the Hela and MCF-7 cancer cell lines show that complexes 1–3 exhibit excellent activity toward the tested tumor cell lines with respect to the standard drug carboplatin, revealing that they have the potential to act as effective metal-based anticancer drugs. 相似文献
120.
Anserinones A and B are natural products that have been shown to have potential anticancer, antifungal, and antibacterial properties. This work entails the novel synthesis of these natural products. 相似文献