Volume 31, Issue 23
Natural Products
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ChemInform Abstract: Two Comparisons of the Performance of Positional Scanning and Deletion Synthesis for the Identification of Active Constituents in Mixture Combinatorial Libraries.

Dale L. Boger

Dale L. Boger

Dep. Chem., Scripps Res. Inst., San Diego, La Jolla, CA 92037, USA

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Jae Kyoo Lee

Jae Kyoo Lee

Dep. Chem., Scripps Res. Inst., San Diego, La Jolla, CA 92037, USA

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Joel Goldberg

Joel Goldberg

Dep. Chem., Scripps Res. Inst., San Diego, La Jolla, CA 92037, USA

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Qing Jin

Qing Jin

Dep. Chem., Scripps Res. Inst., San Diego, La Jolla, CA 92037, USA

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First published: 08 June 2010

Abstract

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ChemInform Abstract

Vitronectin receptor binding inhibition is evaluated with two small libraries of 120 compounds each, which function as Arg-Gly-Asp mimics. Comparison of the performance of positional scanning and deletion synthesis deconvolution libraries to identify active constituents in mixture combinatorial libraries shows that the former is capable of identifying multiple hits at the expense of accurately identifying the most potent library members, i.e. compound (I) for library I and compound (II) for library II, whereas the latter one is more sensitive to identifying the most potent hits (mentioned above) but at the expense of differentiating weaker activities.

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