Discovery of potent, highly selective covalent irreversible BTK inhibitors from a fragment hit.

Hui Qiu, Lesley Liu-Bujalski,Richard D Caldwell,Ariele Viacava Follis,Anna Gardberg,Andreas Goutopoulos,Roland Grenningloh,Jared Head,Theresa Johnson,Reinaldo Jones,Igor Mochalkin,Federica Morandi,Constantin Neagu,Brian Sherer

Bioorganic & Medicinal Chemistry Letters（2018）

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摘要

•A novel series of potent covalent irreversible BTK inhibitors was discovered from a fragment hit.•The optimization of the linker part was accomplished with the aid of MOE.•The top molecule showed comparable cellular potency to ibrutinib and higher kinome selectivity.

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关键词

Covalent,Irreversible,BTK inhibitor,Fragment

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