Modular Synthesis of Radicicol A and Related Resorcylic Acid Lactones, Potent Kinase Inhibitors | Zendy

Dakas PierreYves | Zendy; Barluenga Sofia | Zendy; Totzke Frank | Zendy; Zirrgiebel Ute | Zendy; Winssinger Nicolas | Zendy

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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.

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