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...

Full description

Saved in:
Bibliographic Details
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
Format: Article
Language:English
Subjects:
Chemical microarray
Drug discovery
Library synthesis
Thiol-selective analysis
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary: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.
ISSN:1611-020X
1611-0218
DOI:10.1002/qsar.200640125