Synthesis and anticancer activity of some novel 2-phenazinamine derivatives

被引:36
作者
Gao, Xiaochun [1 ]
Lu, Yuanyuan [1 ]
Fang, Lei [2 ]
Fang, Xubin [2 ]
Xing, Yingying [1 ]
Gou, Shaohua [2 ]
Xi, Tao [1 ]
机构
[1] China Pharmaceut Univ, State Key Lab Nat Med, Nanjing 210009, Jiangsu, Peoples R China
[2] Southeast Univ, Sch Chem & Chem Engn, Pharmaceut Res Ctr, Nanjing 211189, Jiangsu, Peoples R China
关键词
2-Phenazinamine derivatives; Anticancer activity; MTT assay; Apoptosis; CELL PROTECTING SUBSTANCE; IN-VITRO; PHENAZINES; CANCER; ANALOGS; HALIDES; ARYL;
D O I
10.1016/j.ejmech.2013.07.017
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
In this study, we report the synthesis and spectral characterization of a novel series of 2-phenazinamine derivatives. In vitro evaluation for their anticancer activity toward cultured K562 (human chronic myelogenous leukemia), HepG2 (human hepatocellular carcinoma), MGC803 (human gastric carcinoma), HCT116 (human colorectal carcinoma), MCF7 (human breast adenocarcinoma) cell lines, as well as 293T (epithelial cells from human embryo kidney) non-cancer cell was carried out. The compounds 4, 7,16 and 19 showed good positive anticancer activity in vitro. In particular, compound 4, 2-chloro-N-(phenazin-2-yl)benzamide, possessed a potent anticancer effect comparable to cisplatin against both 1<562 and HepG2 cancer cells but was very low or had no effect against 293T non-cancer cell. Preliminary anticancer mechanism of 4 was investigated by cell apoptosis assays compared with cisplatin using flow cytometry. (C) 2013 Elsevier Masson SAS. All rights reserved.
引用
收藏
页码:1 / 9
页数:9
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