Synthesis and Quality Control of Thiol Tagged Compound Libraries for Chemical Microarrays

A method for the synthesis and quality control of compound collections containing reactive thiol functions was developed. Such libraries form the basis for the construction of chemical microarrays to be used in fragment‐based screening. Amino‐modified polymer membranes fixed into the wells of microt...

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Published in:QSAR & combinatorial science 2006-11, Vol.25 (11), p.1047-1054
Main Authors: Maier, Sabine, Frank, Michael, Rau, Harald, Lewandrowski, Peter, Uhrig, Rainer, Keil, Oliver, Deppe, Holger, Müller, Norbert, Vanier, Cecile, Mannsperger, Heiko, Zepter, Siglinde, Junker, Hans-Dieter
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Language:English
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Chemical microarray
Drug discovery
Library synthesis
Thiol-selective analysis
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cited_by cdi_FETCH-LOGICAL-c3275-3ab322c8da131dcec522db924e5156651849dfa8f2b1b50844d99be1a19794913
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container_title QSAR & combinatorial science
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creator Maier, Sabine
Frank, Michael
Rau, Harald
Lewandrowski, Peter
Uhrig, Rainer
Keil, Oliver
Deppe, Holger
Müller, Norbert
Vanier, Cecile
Mannsperger, Heiko
Zepter, Siglinde
Junker, Hans-Dieter
description A method for the synthesis and quality control of compound collections containing reactive thiol functions was developed. Such libraries form the basis for the construction of chemical microarrays to be used in fragment‐based screening. Amino‐modified polymer membranes fixed into the wells of microtiter plates were used as the solid phase for the nanomole‐scale synthesis of a thiol‐tagged small molecule library using a spatial one‐compound/one‐well strategy. A thiolselective Liquid Chromatography‐Mass Spectroscopy (LC‐MS) protocol of each compound before attachment to the microarray surface was established, allowing an exact determination of compound purity and concentration. The established synthesis and quality control method is an important prerequisite for an accurate read‐out of the array compound–target interaction data, and simplifies the usage of small molecule microarrays for low affinity screening.
doi_str_mv 10.1002/qsar.200640125
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subjects Chemical microarray
Drug discovery
Library synthesis
Thiol-selective analysis
title Synthesis and Quality Control of Thiol Tagged Compound Libraries for Chemical Microarrays
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