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A combinatorial scaffold approach toward kinase-directed heterocycle libraries

Academic Article
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Overview

related to degree

  • Wu, Xu, Ph.D. in Chemistry, Scripps Research 2001 - 2004
  • Ding, Sheng, Ph.D. in Chemistry, Scripps Research 1999 - 2003

authors

  • Ding, Sheng
  • Gray, N. S.
  • Wu, Xu
  • Ding, Q.
  • Schultz, Peter

publication date

  • February 2002

journal

  • Journal of the American Chemical Society  Journal

abstract

  • A novel strategy for efficient synthesis of various substituted heterocycles as kinase-directed combinatorial libraries is described. The general scheme involves capture of various dichloroheterocycles onto solid support and further elaborations by aromatic substitution with amines at elevated temperature or by anilines, boronic acids, and phenols via palladium-catalyzed cross-coupling reactions, thus the scaffold itself is transformed into a diversity element within the combinatorial scheme. Libraries consisting of discrete and highly diverse heterocyclic small molecules constructed with these chemistries are currently being evaluated in a variety of cell and protein-based assays.

subject areas

  • Combinatorial Chemistry Techniques
  • Enzyme Inhibitors
  • Heterocyclic Compounds
  • Phosphotransferases
  • Structure-Activity Relationship
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Identity

International Standard Serial Number (ISSN)

  • 0002-7863

Digital Object Identifier (DOI)

  • 10.1021/ja0170302

PubMed ID

  • 11853431
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Additional Document Info

start page

  • 1594

end page

  • 1596

volume

  • 124

issue

  • 8

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