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Modular Synthesis of Radicicol A and Related Resorcylic Acid Lactones, Potent Kinase Inhibitors
Author(s) -
Dakas PierreYves,
Barluenga Sofia,
Totzke Frank,
Zirrgiebel Ute,
Winssinger Nicolas
Publication year - 2007
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.200702406
Subject(s) - kinase , chemistry , trimethylsilyl , modular design , combinatorial chemistry , biochemistry , stereochemistry , computer science , organic chemistry , programming language
Short and sweet : A concise and modular synthesis of radicicol A and related resorcylic acid lactones using fluorous isolation technology and immobilized reagents is reported (see scheme, R F =C 3 H 6 C 6 F 13 , TMSE=2‐(trimethylsilyl)ethyl). The compounds are found to be potent (low‐nanomolar) inhibitors of selected kinases. Despite their irreversible inactivation of kinases, they show good selectivity amongst a panel of 127 kinases.