An efficient one-pot synthesis of heterocycle-fused 1,2,3-triazole derivatives as anti-cancer agents

作者：Yan, Sheng-Jiao; Liu, Yong-Jiang; Chen, Yu-Lan; Liu, Lin; Lin, Jun^*

来源：Bioorganic & Medicinal Chemistry Letters, 2010, 20(17): 5225-5228.

DOI：10.1016/j.bmcl.2010.06.141

• One-pot synthesis
• 1,2,3-Triazole
• Anti-cancer agents

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 mu g/mL against A431 and K562 human tumour cell lines.

• 出版日期2010-9-1
• 单位云南大学