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Molecules 2016, 21(5), 653; doi:10.3390/molecules21050653

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

1
Collaborative Innovation Center of New Drug Research and Safety Evaluation, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China
2
Henan Medical College, Zhengzhou 451191, China
These authors contributed equally to this work.
*
Authors to whom correspondence should be addressed.
Academic Editor: Jean Jacques Vanden Eynde
Received: 10 March 2016 / Revised: 7 May 2016 / Accepted: 12 May 2016 / Published: 19 May 2016
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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. View Full-Text
Keywords: chalcone-1,2,3-triazole-azole; synthesis; antiproliferative; morphological changes chalcone-1,2,3-triazole-azole; synthesis; antiproliferative; morphological changes
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Zhang, S.-Y.; Fu, D.-J.; Yue, X.-X.; Liu, Y.-C.; Song, J.; Sun, H.-H.; Liu, H.-M.; Zhang, Y.-B. Design, Synthesis and Structure-Activity Relationships of Novel Chalcone-1,2,3-triazole-azole Derivates as Antiproliferative Agents. Molecules 2016, 21, 653.

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