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Combinatorial chemistry: A conservative perspective

Combinatorial chemistry: A conservative perspective Large biotechnology based initiatives, like the Human Genome Project, in addition to accelerating scientific progress and improving the understanding of basic biological process, are responsible for an increased demand for high quality drug candidates. In this regard, combinatorial libraries have become a subject of intense interest, as chemists and biologists attempt to generate large numbers of compounds that bind to the increasing number of newly discovered and potentially medically relevant proteins. Now that a variety of exploratory combinatorial chemistry efforts have been reported, it is appropriate to evaluate the utility of these procedures which have often outpaced conservative chemical characterization regarding composition and purity of products. The use of assay formats dictated by the needs of the synthetic protocol have also often circumvented disciplined evaluation of how relevant the assay data is to realistic drug‐target interactions. This commentary examines procedural details whereby commonly used combinatorial practices can generate less useful information than anticipated. Concrete, practical suggestions are made for using combinatorial chemistry in a more focused manner in lead generation and development, so that disappointing results can be avoided and the high potential of this technology more effectively realized. © 1995 Wiley‐Liss, Inc. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Drug Development Research Wiley

Combinatorial chemistry: A conservative perspective

Drug Development Research , Volume 35 (4) – Aug 1, 1995

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References (48)

Publisher
Wiley
Copyright
Copyright © 1995 Wiley‐Liss, Inc.
ISSN
0272-4391
eISSN
1098-2299
DOI
10.1002/ddr.430350404
Publisher site
See Article on Publisher Site

Abstract

Large biotechnology based initiatives, like the Human Genome Project, in addition to accelerating scientific progress and improving the understanding of basic biological process, are responsible for an increased demand for high quality drug candidates. In this regard, combinatorial libraries have become a subject of intense interest, as chemists and biologists attempt to generate large numbers of compounds that bind to the increasing number of newly discovered and potentially medically relevant proteins. Now that a variety of exploratory combinatorial chemistry efforts have been reported, it is appropriate to evaluate the utility of these procedures which have often outpaced conservative chemical characterization regarding composition and purity of products. The use of assay formats dictated by the needs of the synthetic protocol have also often circumvented disciplined evaluation of how relevant the assay data is to realistic drug‐target interactions. This commentary examines procedural details whereby commonly used combinatorial practices can generate less useful information than anticipated. Concrete, practical suggestions are made for using combinatorial chemistry in a more focused manner in lead generation and development, so that disappointing results can be avoided and the high potential of this technology more effectively realized. © 1995 Wiley‐Liss, Inc.

Journal

Drug Development ResearchWiley

Published: Aug 1, 1995

Keywords: chemistry; pharmaceutical; methods

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