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The Contribution of Combinatorial Chemistry to Lead Generation An Interim Analysis

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In the process of finding new drug candidate's medicinal chemists nowadays have a variety of options to choose from, one is to apply combinatorial chemistry techniques. Since the early 1990's synthetic and analytical methods as well as new technologies have been growing repidly in the area of combinatorial chemistry. Applying these techniques have resulted in the production of large numbers of compounds. A trend is observed towards smaller libraries of compounds with more drug-like properties. An analysis is made to establish the contribution of combinatorial chemistry in providing new lead candidates for (pre)clinical development towards new pharmaceutical products. Ten representative examples are given to describe the impact of ombinatorial chemistry on different levels of the lead discovery and optimization process. Furthermore, reports on combinatorial chemistry products that are already in (pre)clinical development were traced back to their source. The interim analysis showed only limied success of combinatorial chemistry approaches in terms of delivering leads. Second generation libraries appear more drug-like and focused and may result in more compounds entering clinical studies in the future
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Keywords: Benzodiazepines; Combinatorial Chemistry; Dansyltyrosine derivatives; Interim Analysis; Phenylstilbene library; Potassium channel blockers; Protein tyrosine kinases; Solid-Phase; Src tyrosine; Thymidylate syntheses Inhibitors

Document Type: Review Article

Publication date: 2001-07-01

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  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.
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