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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

Collaborative Innovation Center of New Drug Research and Safety Evaluation, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China
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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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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