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ky888

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注册: 2008-11-08
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组合化学库的应用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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