Design, synthesis and biological activities of Nilotinib derivates as antitumor agents

被引:19
|
作者
Pan, Xiaoyan [1 ]
Wang, Fang [1 ]
Zhang, Yanmin [1 ]
Gao, Hongping [1 ]
Hu, Zhigang [1 ]
Wang, Sicen [1 ]
Zhang, Jie [1 ]
机构
[1] Xi An Jiao Tong Univ, Coll Med, Xian 710061, Shaanxi Provinc, Peoples R China
关键词
Bcr-Abl; Tyrosine kinase; Leukemia cell; Anticancer; Nilotinib; CHRONIC MYELOGENOUS LEUKEMIA; BCR-ABL; INHIBITORS; DISCOVERY; IMATINIB; AMN107;
D O I
10.1016/j.bmc.2013.02.036
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
A novel class of Nilotinib derivatives, B1-B20, were synthesized in high yields using various substituted anilines. All the title compounds were evaluated for their inhibitory activities against Bcr-Abl and antiproliferative effects on human leukemia cell (K562). The pharmacological results indicated that some compounds exhibited promising anticancer activity. In particular, compound B14 containing tertiary amine side chain exhibited Bcr-Abl inhibitory activity similar to that of Nilotinib. It was suggested that the introduction of the tertiary amine moiety could improve Bcr-Abl inhibitory activity and antitumor effects. (C) 2013 Elsevier Ltd. All rights reserved.
引用
收藏
页码:2527 / 2534
页数:8
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