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

• Main Authors: Sai-Yang Zhang, Dong-Jun Fu, Xiao-Xin Yue, Ying-Chao Liu, Jian Song, Hui-Hui Sun, Hong-Min Liu, Yan-Bing Zhang
• Format: Article
• Language: English
• Published: MDPI AG 2016-05-01
• Series: Molecules
• Subjects: chalcone-1,2,3-triazole-azole; synthesis; antiproliferative; morphological changes
• Online Access: http://www.mdpi.com/1420-3049/21/5/653
• ISSN: 1420-3049

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.