1226548-11-3Relevant academic research and scientific papers
Fused Bicyclic and Tricyclic Pyrimidine Compounds as Tyrosine Kinase Inhibitors
-
Page/Page column 43, (2010/06/11)
Fused bicyclic or tricyclic compounds of formula (I): wherein A, B, C, X, Y, m, and n are defined herein. Also disclosed are a method for inhibiting EGFR kinase activity and a method for treating cancer with these compounds.
Design and synthesis of tetrahydropyridothieno[2,3-d]pyrimidine scaffold based epidermal growth factor receptor (EGFR) kinase inhibitors: The role of side chain chirality and michael acceptor group for maximal potency
Wu, Chia-Hsien,Coumar, Mohane Selvaraj,Chu, Chang-Ying,Lin, Wen-Hsing,Chen, Yi-Rong,Chen, Chiung-Tong,Shiao, Hui-Yi,Rafi, Shaik,Wang, Sing-Yi,Hsu, Hui,Chen, Chun-Hwa,Chang, Chun-Yu,Chang, Teng-Yuan,Lien, Tzu-Wen,Fang, Ming-Yu,Yeh, Kai-Chia,Chen, Ching-Ping,Yeh, Teng-Kuang,Hsieh, Su-Huei,Hsu, John T.-A.,Liao, Chun-Chen,Chao, Yu-Sheng,Hsieh, Hsing-Pang
scheme or table, p. 7316 - 7326 (2011/02/23)
HTS hit 7 was modified through hybrid design strategy to introduce a chiral side chain followed by introduction of Michael acceptor group to obtain potent EGFR kinase inhibitors 11 and 19. Both 11 and 19 showed over 3 orders of magnitude enhanced HCC827 a
