Synthesis and antitumor activity of water-soluble poly(aminoheterocyclic amine)s (I):: N,N,N′,N′-tetra[2-(4-amino-5-substituted-s-triazol-3-yl sulfanyl)ethyl]-1,4-benzyldiamine salts

被引:5
作者
Hu, Guo Qiang [1 ]
Xie, Song Qiang
Huang, Wen Long
机构
[1] Henan Univ, Inst Pharm, Kaifeng 475001, Peoples R China
[2] China Pharmaceut Univ, Nanjing 210009, Peoples R China
基金
中国国家自然科学基金;
关键词
triazole; polyamine; water-soluble; antitumor activity;
D O I
10.1016/j.cclet.2006.12.001
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Five water-soluble poly(aminoheterocyclic amine)s containing s-triazole ring were synthesized as respective HCl salts (5a-5e). Biological activities in L1210 (murine leukemia) and Chinese hamster ovary (CHO) cell lines were investigated via IC50 cytotoxicity determinations. The title compounds represented moderate cytotoxicity (low IC50 values between 15 and 68 mu mol/L) in L1210 but high cytotoxicity (lower IC50 values: 0.25, 0.018, 0.014 mu mol/L for 5a-5e, respectively) in CHO cell lines, while the corresponding HCl salts of the intermediates (3a-3e) without polyamine tether and starting materials amino-s-triazoles (la-le) showed poor or no activities against the above cell lines. (c) 2006 Guo Qiang Hu. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved.
引用
收藏
页码:124 / 126
页数:3
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