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Scientific article
English

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

Contributors

Moulin, Emilie; Barluenga, Sofia; Totzke, Frank; Winssinger, Nicolas

Published in

Chemistry, vol. 12, no. 34, p. 8819-8834

Publication date

2006

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

UNIGE 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

Main files (1)

Article (Published version)

Identifiers

Journal ISSN

0947-6539
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Technical informations

Creation

11/12/2012 17:14:00

First validation

11/12/2012 17:14:00

Update

13/10/2025 23:53:11

Status update

14/03/2023 17:47:15

Last indexation

01/07/2026 06:09:23
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