Synthesis of Novel Antiproliferative 1, 2, 3-triazole Hybrids Using the Molecular Hybridisation Approach. (November 2016)

• Record Type: Journal Article
• Authors: Fu, Dong-Jun; Song, Jian; Zhao, Ruo-Han; Liu, Ying-Chao; Zhang, Yan-Bing; Liu, Hong-Min
• Is Part Of: Journal of chemical research. Volume 40:Number 11(2016)
• Page Start: 674
• Page End: 677
• Publication Date: 2016-11
• Subjects: 1, 2, 3-triazole -- chalcone -- molecular hybridisation -- antiproliferative; Chemistry -- Research -- Periodicals; Chemistry -- Periodicals; 540.5
• DOI: 10.3184/174751916X14761050193688
• Languages: English
• ISSNs: 1747-5198

Abstract

A series of nine novel 1, 2, 3-triazole-chalcone derivatives were designed using the molecular hybridisation approach and synthesised by click chemistry. Most of the synthesised compounds exhibited moderate to good antiproliferative activity against oesophagus, gastric and neuroendocrine cancer cell lines, but a compound containing a p-bromo group in the A ring and a [(4, 5-dihydrothiazol-2-yl)thio]methyl group attached at the 4-position of a p-[3-(1, 2, 3-triazol-1-yl)propyloxy] group in the B ring showed the highest activity with an IC50 value of 8.16 μM against neuroendocrine cancer cells. The structure activity relationships of all nine compounds were discussed.