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Molecular Editing of Kinase‐Targeting Resorcylic Acid Lactones (RAL): Fluoroenone RAL
Author(s) -
Jogireddy Rajamalleswaramma,
Barluenga Sofia,
Winssinger Nicolas
Publication year - 2010
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201000047
Subject(s) - pharmacophore , kinome , kinase , biochemistry , small molecule , chemistry , cysteine , biology , stereochemistry , enzyme
Molecular editing : The resorcylic acid lactones (RAL) are known small‐molecule irreversible inhibitors of select kinases, and represent a unique pharmacophore with potential for further development in kinase research. The basic pharmacophore was “edited” to improve the properties and to diversify the scaffold. Two fluoroenones were synthesized, and their preliminary biological evaluation revealed interesting activity.