title: Design, Synthesis and Structure-Activity Relationships of Novel Chalcone-1,2,3-triazole-azole Derivates as Antiproliferative Agents.
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.
authors.affiliation: Collaborative Innovation Center of New Drug Research and Safety Evaluation, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China. celeron16@163.com.
authors.forename: Sai-Yang
authors.initials: SY
authors.lastname: Zhang
authors.affiliation: Collaborative Innovation Center of New Drug Research and Safety Evaluation, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China. Fudongjun@gs.zzu.edu.cn.
authors.forename: Dong-Jun
authors.initials: DJ
authors.lastname: Fu
authors.affiliation: Henan Medical College, Zhengzhou 451191, China. xxyue1115@126.com.
authors.forename: Xiao-Xin
authors.initials: XX
authors.lastname: Yue
authors.affiliation: Collaborative Innovation Center of New Drug Research and Safety Evaluation, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China. zzulyc@163.com.
authors.forename: Ying-Chao
authors.initials: YC
authors.lastname: Liu
authors.affiliation: Collaborative Innovation Center of New Drug Research and Safety Evaluation, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China. mumuandzz@163.com.
authors.forename: Jian
authors.initials: J
authors.lastname: Song
authors.affiliation: Collaborative Innovation Center of New Drug Research and Safety Evaluation, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China. 15937152262@163.com.
authors.forename: Hui-Hui
authors.initials: HH
authors.lastname: Sun
authors.affiliation: Collaborative Innovation Center of New Drug Research and Safety Evaluation, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China. liuhm@zzu.edu.cn.
authors.forename: Hong-Min
authors.initials: HM
authors.lastname: Liu
authors.affiliation: Collaborative Innovation Center of New Drug Research and Safety Evaluation, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China. zhangyb@zzu.edu.cn.
authors.forename: Yan-Bing
authors.initials: YB
authors.lastname: Zhang
mesh_terms: D001393:Azoles / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D006801:Humans; D013329:Structure-Activity Relationship
chemical_list: D001393:Azoles
keywords: antiproliferative; chalcone-1,2,3-triazole-azole; morphological changes; synthesis