1192181-52-4Relevant academic research and scientific papers
An efficient one-pot synthesis of heterocycle-fused 1,2,3-triazole derivatives as anti-cancer agents
Yan, Sheng-Jiao,Liu, Yong-Jiang,Chen, Yu-Lan,Liu, Lin,Lin, Jun
experimental part, p. 5225 - 5228 (2010/10/01)
A series of heterocycle-fused 1,2,3-triazoles were easily prepared by the 1,3-dipolar cycloaddition of heterocyclic ketene aminals or N,O-acetals with sodium azide and polyhalo isophthalonitriles in a one-pot reaction at room temperature without a catalyst and evaluated in vitro against a panel of human tumour cell lines. 1,3-Oxazoheterocycle fused 1,2,3-triazoles were more potent against the tumour cell lines Skov-3, HL-60, A431, A549 and HepG-2 than 1,3-diazoheterocycle fused 1,2,3-triazoles. 4-Methoxyphenyl substituted 1,3-oxazoheterocycle fused 1,2,3-triazole 6j was found to be the most potent derivative with IC50 values lower than 1.9 μg/mL against A431 and K562 human tumour cell lines.
