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Synthesis of a Resorcylic Acid Lactone (RAL) Library Using Fluorous‐Mixture Synthesis and Profile of its Selectivity Against a Panel of Kinases
Author(s) -
Jogireddy Rajamalleswaramma,
Dakas PierreYves,
Valot Gaëlle,
Barluenga Sofia,
Winssinger Nicolas
Publication year - 2009
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.200901375
Subject(s) - moiety , selectivity , kinase , pharmacophore , chemistry , residue (chemistry) , stereochemistry , combinatorial chemistry , biochemistry , catalysis
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.