Synthesis of novel antiproliferative 1,2,3-triazole hybrids using the molecular hybridisation approach
Synthesis of novel antiproliferative 1,2,3-triazole hybrids using the molecular hybridisation approach
复制标题
使用分子杂交方法合成新型抗增殖 1,2,3-三唑杂化物
DOI：
10.3184/174751916x14761050193688
复制
发表时间：
2016-11-01
影响因子：
1.4
通讯作者：
Liu, Hong-Min
中科院分区：
文献类型：
--
作者：
Fu, Dong-Jun;Song, Jian;Liu, Hong-Min
利用分子杂交技术设计并合成了9个新的1，2，3-三唑查尔酮衍生物。大多数合成的化合物对食管癌、胃癌和神经内分泌癌细胞系表现出中等至良好的抗增殖活性，但在A环中含有对溴基团和[（4，5-二氢噻唑-2-基）硫代]甲基，其连接在对-[3-（三氟甲基）苯基]-N-（4，5-二氢噻唑-2-基）硫代]甲基的4-位。B环上的[（1，2，3-三唑-1-基）丙氧基]对神经内分泌癌细胞显示出最高活性，IC 50值为8.16 μM。讨论了9个化合物的构效关系。
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.