引用本文:
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
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
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
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
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 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.
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关键词:
- Triazole
- / Polyamine
- / Water-soluble
- / Antitumor activity
English
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
Abstract:
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.
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Key words:
- Triazole
- / Polyamine
- / Water-soluble
- / Antitumor activity
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