Citation: Guo Qiang Hu, Song Qiang Xie, Wen Long Huang. 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[J]. Chinese Chemical Letters, ;2007, 18(2): 124-126. doi: 10.1016/j.cclet.2006.12.001 shu

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

a Institute of Pharmacy, Henan University, Kaifeng 475001, China;
b China Pharmaceutical University, Nanjing 210009, China

Received Date: 5 July 2006

Fund Project: This project was supported by National Natural Science Foundation of China (No. 30070861) and the Science Foundation of Henan University (04ZDZR009).

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 IC₅₀cytotoxicity determinations. The title compounds represented moderate cytotoxicity (low IC₅₀ values between 15 and 68 μmol/L)in L1210 but high cytotoxicity (lower IC₅₀ values:0.25, 0.018, 0.014 μmol/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 (1a-1e)showed poor or no activities against the above cell lines.
- Triazole,
- Polyamine,
- Water-soluble,
- Antitumor activity
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