Correlation of structural features of novel 1,2,3-triazoles with their neurotoxic and tumoricidal properties.

Triazoles are interesting templates for novel chemotherapeutic drugs. We synthesized here 17 1,3,4-substituted-1,2,3-triazoles that differed in their 1'-substituent (variable alkyl chain lengths C3-C12), the 3'-substituent (no substituent, -methyl or -propyl) or the salt form obtained. Several of the compounds were cytotoxic (μM range) for tumor cells (HL-60, Jurkat, MCF-7, HCT-116), and when the effect was compared to non-transformed cells (Vero), selectivity ratios of up to 23-fold were obtained.

Synthesis and biological evaluation of some 6-substituted purines.

We report herein the synthesis and the in vitro antileishmanial evaluation of a series of 6-substituted purines. The most active compounds against Leishmania amazonensis promastigotes were 6-(3'-chloropropylthio)purine 2 [11,12] [corrected] 6-(3'-(thioethylamine)propylthio)purine 5, 6-(alpha-aceticacidthio)purine 7 and 6-(6'-deoxy-1'-O-methyl-beta-D-ribofuranose)purine 14 with an IC(50)=50, 50, 39 and 29 microM, respectively.