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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

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
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摘要 Five water-soluble poly(aminoheterocyclic amine)s containing s-triazole ring were synthesized as respective HC1 salts (5a-5e). Biological activities in L1210 (murine leukemia) and Chinese hamster ovary (CHO) cell lines were investigated via IC50 cytotoxicity determinations. The tide compounds represented moderate cytotoxicity (low IC50 values between 15 and 68μmol/L) in L1210 but high cytotoxicity (lower IC50 values: 0.25,0.018,0.014μmol/L for Sa-5e, respectively) in CHO cell lines, while the corresponding HC1 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. Five water-soluble poly(aminoheterocyclic amine)s containing s-triazole ring were synthesized as respective HC1 salts (5a-5e). Biological activities in L1210 (murine leukemia) and Chinese hamster ovary (CHO) cell lines were investigated via IC50 cytotoxicity determinations. The tide compounds represented moderate cytotoxicity (low IC50 values between 15 and 68μmol/L) in L1210 but high cytotoxicity (lower IC50 values: 0.25,0.018,0.014μmol/L for Sa-5e, respectively) in CHO cell lines, while the corresponding HC1 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.
出处 《Chinese Chemical Letters》 SCIE CAS CSCD 2007年第2期124-126,共3页 中国化学快报(英文版)
关键词 TRIAZOLE POLYAMINE WATER-SOLUBLE Antitumor activity Triazole Polyamine Water-soluble Antitumor activity
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参考文献1

  • 1Tomio Takeuchi.Antitumor antibiotics discovered and studied at the Institute of Microbial Chemistry[J].Journal of Cancer Research and Clinical Oncology (-).1995(9-10)

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