6-Substituted 1,4-Naphthoquinone Oxime Derivatives (III): Synthesis and Cytotoxic Evaluation

被引：3
|
作者：
Huang, G. [1 ]
Liu, M. C. [1 ]
Meng, Q. Q. [1 ]
Li, S. S. [1 ]
机构：
[1] Shanghai Jiao Tong Univ, Sch Pharm, Shanghai 200240, Peoples R China
来源：
RUSSIAN JOURNAL OF GENERAL CHEMISTRY | 2018年 / 88卷 / 05期
基金：
中国国家自然科学基金;
关键词：
1,4-naphthoquinone; oxime derivatives; drug research; structure-activity relationships; cytotoxic activity; AGENTS;
D O I：
10.1134/S1070363218050316
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
As a continuous study, a set of 23 new 6-substituted 1,4-naphthoquinone oxime derivatives are synthesized and screened for their in vitro cytotoxic activity. Four of those oxime derivatives demonstrate more potent cytotoxic activity towards K562, HCT-15, and HCT-116 cell lines than a reference drug 5-Fu. In particular, compound 21g exhibits the strongest inhibitory activity against K562 cell lines with IC50 values of 1.25 mu M. According to flow cytometry data, compound 21g can arrest cell cycle at S phase and induce a strong apoptotic response in K562 cells. The preliminary structure-activity relationship study shows that the nature of substituents in positions 6 and 1' of 1,4-naphthoquinone derivatives significantly affect their cytotoxic activity.
引用
收藏
页码：1025 / 1035
页数：11
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