Synthesis of a Resorcylic Acid Lactone (RAL) Library Using Fluorous‐Mixture Synthesis and Profile of its Selectivity Against a Panel of Kinases |
| |
| Authors: | Rajamalleswaramma Jogireddy Pierre‐Yves Dakas Gaëlle Valot Sofia Barluenga Nicolas Winssinger |
| |
| Affiliation: | Institut de Science et Ingénierie Supramoléculaires (ISIS–UMR 7006), Université de Strasbourg—CNRS, 8 allée Gaspard Monge, 67000 Strasbourg (France), Fax. (+33)?368‐855‐113 |
| |
| Abstract: | 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. |
| |
| Keywords: | combinatorial chemistry fluorous chemistry kinases lactones resorcylic acid |
|
