Synthesis and biological evaluation of pyrimidine-based dual inhibitors of human epidermal growth factor receptor 1 (HER-1) and HER-2 tyrosine kinases

…, SJ Kang, YH Jung, JY Song, KJ Choi…

文献索引：Cha, Mi Young; Lee, Kwang-Ok; Kang, Seok-Jong; Jung, Young Hee; Song, Ji Yeon; Choi, Kyung Jin; Byun, Joo Yun; Lee, Han-Jae; Lee, Gwan Sun; Park, Seung Bum; Kim, Maeng Sup Journal of Medicinal Chemistry, 2012 , vol. 55, # 6 p. 2846 - 2857

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被引用次数: 15

摘要

A novel series of N 4-(3-chlorophenyl)-5-(oxazol-2-yl) pyrimidine-4, 6-diamines were synthesized and evaluated as dual inhibitors of HER-1/HER-2 tyrosine kinases. In contrast to the currently approved HER-2-targeted agent (lapatinib, 1), our irreversible HER-1/HER-2 inhibitors have the potential to overcome the clinically relevant and mutation-induced drug resistance. The selected compound (19a) showed excellent inhibitory activity toward HER ...