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October 5, 2010Journal of Combinatorial Chemistry

Comprehensive Survey of Chemical Libraries for Drug Discovery and Chemical Biology: 2009

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Authors

RDRoland E. DolleWashington University in St. LouisBBBertrand Le BourdonnecDeciphera Pharmaceuticals (United States)KWKarin WormBristol-Myers Squibb (Germany)

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Implication

Literature review reveals global progress in chemical library synthesis for biological targets, highlighting strategies to enhance lead optimization in drug discovery.

Key Points

  • To review the design, synthesis, and screening applications of small-molecule chemical libraries published throughout 2009 for drug discovery and chemical biology.
  • Surveyed peer-reviewed literature published in 2009 focused on combinatorial and parallel chemical library synthesis.
  • Classified synthetic small-molecule collections by scaffold class, reaction methodology, and biological target families including receptors and enzymes.
  • Outlined synthetic library methodologies yielding novel antagonists, enzyme inhibitors, and functional probes for biological validation.
  • Identified trends toward diversity-oriented synthesis and target-directed libraries to improve compound quality for high-throughput screening campaigns.

Cite This Study

Dolle et al. (2010) studied this question.

synapsesocial.com/papers/6a0c67b1e28175e95a234e24https://doi.org/10.1021/cc100128w
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