Scientific article
English

Diversity-Oriented Synthesis of Pochonins and Biological Evaluation against a Panel of Kinases

Published inChemistry, vol. 12, no. 34, p. 8819-8834
Publication date2006
Abstract

Pochonins A–F were recently characterized as six new members of the naturally occurring family of 14-membered resorcylic acid lactones. As there are a high number of ATPase and kinase inhibitors among natural resorcylic lactones, a library based on the pochonin scaffold, with five points of diversity, was prepared which includes diversity beyond that of the natural analogues. The library was synthesized by using solid-supported reagents amenable to automation. Testing the library for its inhibition against a panel of 24 kinases at 10 μm afforded a >14 % hit rate. These results demonstrate the potential of the resorcylides towards the inhibition of therapeutically relevant kinases.

Keywords
  • Bergerat fold
  • combinatorial chemistry
  • kinase inhibitors
  • organic synthesis
  • pochonin
Affiliation entities Not a UNIGE publication
Citation (ISO format)
MOULIN, Emilie et al. Diversity-Oriented Synthesis of Pochonins and Biological Evaluation against a Panel of Kinases. In: Chemistry, 2006, vol. 12, n° 34, p. 8819–8834. doi: 10.1002/chem.200600553
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Article (Published version)
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Identifiers
Journal ISSN0947-6539
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