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Diversity‐Oriented Synthesis of Pochonins and Biological Evaluation against a Panel of Kinases
Author(s) -
Moulin Emilie,
Barluenga Sofia,
Totzke Frank,
Winssinger Nicolas
Publication year - 2006
Publication title -
chemistry – a european journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.687
H-Index - 242
eISSN - 1521-3765
pISSN - 0947-6539
DOI - 10.1002/chem.200600553
Subject(s) - kinase , diversity (politics) , protein serine threonine kinases , chemistry , biochemistry , biology , computational biology , protein kinase a , political science , law
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 μ M afforded a >14 % hit rate. These results demonstrate the potential of the resorcylides towards the inhibition of therapeutically relevant kinases.