期刊
CHEMISTRY-A EUROPEAN JOURNAL
卷 15, 期 43, 页码 11498-11506出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/chem.200901375
关键词
combinatorial chemistry; fluorous chemistry; kinases; lactones; resorcylic acid
资金
- Agence National de la Recherche (ANR)
- Conectus
- MNRT
- ARC
A library of resorcylic acid lactones (RAL) containing a cis-enone moiety targeting kinases hearing a cysteine residue within the ATP-binding pocket was prepared using a fluorous-mixture synthesis and evaluated against a panel of 19 kinases thus providing important structure-activity trends. Two new analogues were then profiled for their selectivity against a panel of 402 kinases providing the broadest evaluation of this pharmacophores' selectivity
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