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Title

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

Authors
Moulin, Emilie
Barluenga, Sofia
Totzke, Frank
Published in Chemistry - A European Journal. 2006, vol. 12, no. 34, p. 8819-8834
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 foldcombinatorial chemistrykinase inhibitorsorganic synthesispochonin
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Other version: http://doi.wiley.com/10.1002/chem.200600553
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MOULIN, Emilie et al. Diversity-Oriented Synthesis of Pochonins and Biological Evaluation against a Panel of Kinases. In: Chemistry - A European Journal, 2006, vol. 12, n° 34, p. 8819-8834. https://archive-ouverte.unige.ch/unige:24529

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Deposited on : 2012-12-12

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