Synthesis and biological evaluation of quinoline derivatives as potential anti-prostate cancer agents and Pim-1 kinase inhibitors
Synthesis and biological evaluation of quinoline derivatives as potential anti-prostate cancer agents and Pim-1 kinase inhibitors
复制标题
喹啉衍生物作为潜在抗前列腺癌药物和 Pim-1 激酶抑制剂的合成和生物学评价
DOI：
10.1016/j.bmc.2016.03.016
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发表时间：
2016-04-15
影响因子：
3.5
通讯作者：
Zhao, Linxiang
中科院分区：
文献类型：
--
作者：
Li, Kun;Li, Ying;Zhao, Linxiang
In this work, a series of quinoline derivatives were designed and synthesized as antitumor agents. Most quinolines showed potent anti-proliferative activity against human prostatic cancer PC-3 cell line. Among which, 9d, 9f and 9g were the most effective compounds with GI(50) values of 2.60, 2.81 and 1.29 mu M, respectively. Structure-activity relationship analysis indicated that the secondary amine linked quinoline and pyridine ring played an important role in the anti-proliferative effects. Mechanistic studies revealed that 9g was a potential Pim-1 kinase inhibitor with abilities of cell cycle arrest and apoptosis induction. Considering of the increased activity of Pim-1 in prostate cancer, such compounds have potential to be developed as anti-prostate cancer agents. (C) 2016 Published by Elsevier Ltd.
