Design, Synthesis and Structure-Activity Relationships of Novel Chalcone-1,2,3-triazole-azole Derivates as Antiproliferative Agents

Molecules. 2016 May 19;21(5):653. doi: 10.3390/molecules21050653.

Abstract

A series of novel chalcone-1,2,3-triazole-azole hybrids were designed, synthesized and evaluated for their antiproliferative activity against three selected cancer cell lines (SK-N-SH, EC-109 and MGC-803). Most of the synthesized compounds exhibited moderate to good activity against all the cancer cell lines selected. Particularly, compound I-21 showed the most excellent antiproliferative activity with an IC50 value of 1.52 μM against SK-N-SH cancer cells. Further mechanism studies revealed that compound I-21 induced morphological changes of SK-N-SH cancer cells possibly by inducing apoptosis. Novel chalcone-1,2,3-triazole-azole derivatives in this work might be a series of promising lead compounds to develop anticancer agents for treating neuroblastoma.

Keywords: antiproliferative; chalcone-1,2,3-triazole-azole; morphological changes; synthesis.

MeSH terms

  • Azoles / chemistry*
  • Azoles / pharmacology*
  • Cell Line, Tumor
  • Humans
  • Structure-Activity Relationship

Substances

  • Azoles