Chemistry - A European Journal p. 11498 - 11506 (2009)
Update date:2022-09-26
Topics:
Jogireddy, Rajamalleswaramma
Dakas, Pierre-Yves
Valot, Gaelle
Barluenga, Sofia
Winssinger, Nicolas
A library of resorcylic acid lactones (RAL) containing a cis-enone moiety targeting kinases bearing 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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