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  • Title: Diversity-oriented synthesis of pochonins and biological evaluation against a panel of kinases.
    Author: Moulin E, Barluenga S, Totzke F, Winssinger N.
    Journal: Chemistry; 2006 Nov 24; 12(34):8819-34. PubMed ID: 16953513.
    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 microM afforded a >14 % hit rate. These results demonstrate the potential of the resorcylides towards the inhibition of therapeutically relevant kinases.
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