The discovery of highly selective erbB2 (Her2) inhibitors for the treatment of cancer.

Blaise Lippa,Goss S Kauffman,Joel Arcari,Tricia Kwan,Jinshan Chen,William Hungerford,Samit Bhattacharya,Xumiao Zhao,Courtney Williams,Jun Xiao,Leslie Pustilnik,Chunyan Su,James D Moyer,Ling Ma,Mary Campbell,Stefanus Steyn

Bioorganic & Medicinal Chemistry Letters（2007）

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摘要

The synthesis and biological evaluation of potent and selective inhibitors of the erbB2 kinase is presented. The vast majority of these compounds are found to be >100× selective over the closely related EGFR kinase. Two lead compounds are further shown to have low clearance and moderate bioavailability in rat.

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关键词

erbB2,Her2,Anilinoquinazoline,Kinase,Cancer

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