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

…, T Kwan, J Chen, W Hungerford, S Bhattacharya…

Index: 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 Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 11 p. 3081 - 3086

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Citation Number: 18

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 pyrido [4, 3-d] pyrimidine cores. 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 ...