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

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.

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

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 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.