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Keggin结构钨磷酸稀土镨盐杂多蓝的合成及抗艾滋病病毒(HIV-1)活性的研究 总被引:9,自引:0,他引:9
Keggin结构钨磷酸稀土镨盐杂多蓝的合成及抗艾滋病病毒(HIV-1)活性的研究刘术侠,刘彦勇,王恩波,曾毅,李泽琳(东北师范大学化学系,长春,130024)(中国预防医学科学院,北京)关键词稀土,钨磷杂多蓝,合成,抗艾滋病病毒(HIV-1)活性杂多... 相似文献
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Ficarra P. Ficarra R. Chimirri A. Romeo G. Tommasini S. Calabrò M. L. Costantino D. Monforte A. M. Carulli M. 《Chromatographia》1994,38(1-2):57-61
Summary Anti-HIV enantiomeric 1H, 3H-thiazolo[3, 4-a] benzimidazoles have been stereospecifically analyzed by elution on a column of cellulose tris-(4-methyl-phenylbenzoate)ester adsorbed on macroporous silica (ChiralcelR OJ).The enantiomeric resolution of the compounds examined is linked to a complex and competitive contribution of different factors. 相似文献
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新型稀土杂多蓝的合成及其抗艾滋病病毒(HIV-1)活性和毒性研究 总被引:14,自引:0,他引:14
合成Keggin结构钨硅、钨锗、钨磷、钨坤两电子及四电子稀土钐盐杂多蓝,铈量滴定及元素分析方法确定了化合物的还原电子数及化学组成,采用IR,UV-Vis,^183W NMR和ESR等对其结果进行了表征,在人T淋巴MT-4内,对合成的化合物进行了系统的抗艾滋病毒(HIV-1)活性及毒性测定,发现Keggin结构钨硅、钨锗四电子稀土钐盐杂多蓝具有较强的抗HIV-1活性,其中钨锗酸钐四电子杂多蓝(代号HPBR-2)具有较高的治疗指数。 相似文献
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Qian Wang Assoc. Prof. Fuhang Song Dr. Xue Xiao Pei Huang Assoc. Prof. Li Li Prof. Aaron Monte Dr. Wael M. Abdel‐Mageed Dr. Jian Wang Hui Guo Dr. Wenni He Feng Xie Dr. Huanqin Dai Miaomiao Liu Dr. Caixia Chen Hao Xu Assoc. Prof. Mei Liu Dr. Andrew M. Piggott Assoc. Prof. Xueting Liu Prof. Robert J. Capon Prof. Lixin Zhang 《Angewandte Chemie (International ed. in English)》2013,52(4):1231-1234
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Synthesis and Biological Evaluation of RGD Peptidomimetic–Paclitaxel Conjugates Bearing Lysosomally Cleavable Linkers
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Alberto Dal Corso Dr. Michele Caruso Dr. Laura Belvisi Dr. Daniela Arosio Prof. Dr. Umberto Piarulli Dr. Clara Albanese Dr. Fabio Gasparri Dr. Aurelio Marsiglio Dr. Francesco Sola Dr. Sonia Troiani Dr. Barbara Valsasina Dr. Luca Pignataro Dr. Daniele Donati Prof. Dr. Cesare Gennari 《Chemistry (Weinheim an der Bergstrasse, Germany)》2015,21(18):6921-6929
Two small‐molecule–drug conjugates (SMDCs, 6 and 7 ) featuring lysosomally cleavable linkers (namely the Val–Ala and Phe–Lys peptide sequences) were synthesized by conjugation of the αvβ3‐integrin ligand cyclo[DKP–RGD]‐CH2NH2 ( 2 ) to the anticancer drug paclitaxel (PTX). A third cyclo[DKP–RGD]–PTX conjugate with a nonpeptide “uncleavable” linker ( 8 ) was also synthesized to be tested as a negative control. These three SMDCs were able to inhibit biotinylated vitronectin binding to the purified αVβ3‐integrin receptor at nanomolar concentrations and showed good stability at pH 7.4 and pH 5.5. Cleavage of the two peptide linkers was observed in the presence of lysosomal enzymes, whereas conjugate 8 , which possesses a nonpeptide “uncleavable” linker, remained intact under these conditions. The antiproliferative activities of the conjugates were evaluated against two isogenic cell lines expressing the integrin receptor at different levels: the acute lymphoblastic leukemia cell line CCRF‐CEM (αVβ3?) and its subclone CCRF‐CEM αVβ3 (αVβ3+). Fairly effective integrin targeting was displayed by the cyclo[DKP–RGD]–Val–Ala–PTX conjugate ( 6 ), which was found to differentially inhibit proliferation in antigen‐positive CCRF‐CEM αVβ3 versus antigen‐negative isogenic CCRF‐CEM cells. The total lack of activity displayed by the “uncleavable” cyclo[DKP–RGD]–PTX conjugate ( 8 ) clearly demonstrates the importance of the peptide linker for achieving the selective release of the cytotoxic payload. 相似文献
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Najim A. Al-Masoudi Nazik M. Aziz Abdulalah T. Mohammed 《Phosphorus, sulfur, and silicon and the related elements》2013,188(11):2891-2901
New Schiff base ligands (6–9) derived from 5-amino-4-phenyl-4H-1,2,4-triazole-3-thiol 1 and substituted benzaldehydes (2–5) as well as their metal complexes with Cu(II), Fe(II), Au(III), and Mn(II) (12–17) have been synthesized. A new benzothiazole derivative (11) was prepared from coupling of 7 with N-(benzothiazol-2-yl)-2-chloroacetamide 10. Their spectral properties were investigated. The newly designed and synthesized Schiff base ligands and the metal complexes were assayed for anti-HIV-1 and HIV-2 activity by examination of their inhibition of HIV-induced cytopathogenicity in MT-4 cells. Compounds 11 and 16 were found to be the most active inhibitors in cell culture (EC50 = 12.2 μg/mL (SI = 4) and > 2.11 μg/mL (SI = > 1), respectively) against HIV-1, whereas 11 showed inhibition against HIV-2 of EC50 > 10.2 μg/mL with SI = 9, which provided a good lead for further optimization. 相似文献
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Nikolaus Krall Dr. Jörg Scheuermann Prof. Dario Neri 《Angewandte Chemie (International ed. in English)》2013,52(5):1384-1402
The targeted delivery of potent cytotoxic agents has emerged as a promising strategy for the treatment of cancer and other serious conditions. Traditionally, antibodies against markers of disease have been used as drug‐delivery vehicles. More recently, lower molecular weight ligands have been proposed for the generation of a novel class of targeted cytotoxics with improved properties. Advances in this field crucially rely on efficient methods for the identification and optimization of organic molecules capable of high‐affinity binding and selective recognition of target proteins. The advent of DNA‐encoded chemical libraries allows the construction and screening of compound collections of unprecedented size. In this Review, we survey developments in the field of small ligand‐based targeted cytotoxics and show how innovative library technologies will help develop the drugs of the future. 相似文献