Structural optimization of diphenylpyrimidine derivatives (DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors with improved activity toward B leukemia cell lines

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• 作者：Dan Zhao^a ; Shanshan Huang^a ; Menghua Qu^a ; Changyuan Wang^a ; Zhihao Liu^a ; Zhen Li^a ; Jinyong Peng^a ; Kexin Liu^a ; Yanxia Li^b ; Xiaodong Ma^a ; ^{xiaodong.ma@139.com} ; Xiaohong Shu^a ; ^{xiaohong_shu@dmu.edu.cn}
• 关键词：Leukemia ; BTK ; Pyrimidine ; Synthesis ; Inhibitor
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：27 January 2017
• 年：2017
• 卷：126
• 期：Complete
• 页码：444-455
• 全文大小：3425 K
• 卷排序：126

文摘

A new series of DPPYs were synthesized and biologically evaluated as potent BTK inhibitors. DPPYs could inhibit BTK activity at nanomolar concentrations. Inhibitor 7j displayed higher inhibitory capacity to interfere with B leukemia cell lines than ibrutinib. Inhibitor 7j has low cell cytotoxicity against normal PBMC cells.