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The discovery of highly selective erbB2 (Her2) inhibitors for the treatment of cancer
Authors:Lippa Blaise  Kauffman Goss S  Arcari Joel  Kwan Tricia  Chen Jinshan  Hungerford William  Bhattacharya Samit  Zhao Xumiao  Williams Courtney  Xiao Jun  Pustilnik Leslie  Su Chunyan  Moyer James D  Ma Ling  Campbell Mary  Steyn Stefanus
Institution:Pfizer, Inc., PGRD Groton, MS-8220-2203 Eastern Point Road, Groton, CT 06340, USA. blaise.lippa@pfizer.com
Abstract:The synthesis and biological evaluation of potent and selective inhibitors of the erbB2 kinase is presented. Based on the 4-anilinoquinazoline chemotype, the syntheses of several new series of erbB2 inhibitors are described with quinazoline and pyrido4,3-d]pyrimidine cores. The vast majority of these compounds are found to be >100x 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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