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ky888銀蟲 (正式寫手)
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[求助]
幫忙翻譯下吧 不懂啊
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組合化學庫的應用Library applications The electrochemical behaviour of an indole library of compounds, including several tryptophan and tryptamine derivatives previously demonstrated to be active against reactive oxygen species (ROS), has been investigated. A voltammetry study has been undertaken and the oxidation potential was correlated to the scavenging activity reported for these indoles.9 Tripeptides such as RGD and NGR are showing promising results for targeted drug delivery and in vivo imaging. An on resin Huisgen’s 1,3-dipolar cycloaddition has been used to synthesise new cyclic RGD and NGR peptide analogues and preliminary binding assays of these new analogues by fluorescence polarisation indicated specific binding to purified CD13 (Aminopeptidase N) and cell lysates from MCF-7 and SKOV-3 cancer cell lines.10 A novel series of quinolinone-based adenosine A2B receptor antagonists has been identified via high throughput screening of an encoded combinatorial compound collection. Synthesis and assay of a series of analogues highlighted essential structural features of the initial hit, and subsequent optimisation resulted in an A2B antagonist which exhibited potent activity in cAMP accumulation and IL-8 release assays.11 Screening of a pteridine-based compound library led to the identification of compounds exhibiting immunosuppressive as well as anti-inflammatory activity. Optimisation afforded a series of 2-amino- 4-N-piperazinyl-6-(3,4-dimethoxyphenyl)pteridine analogues, the most potent of which displayed low nM IC50 values in the Mixed Lymphocyte Reaction (MLR) assay.12 |
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ky888
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ky888
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