Synthesis of a Resorcylic Acid Lactone (RAL) Library Using Fluorous‐Mixture Synthesis and Profile of its Selectivity Against a Panel of Kinases | Zendy

Jogireddy Rajamalleswaramma | Zendy; Dakas PierreYves | Zendy; Valot Gaëlle | Zendy; Barluenga Sofia | Zendy; Winssinger Nicolas | Zendy

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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.

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