摘要
为了寻找结构新颖的生物活性分子,采用活性亚结构拼接原理设计合成了12个哌嗪取代呋喃查尔酮衍生物(3a^3l),其结构经~1H NMR、^(13)C NMR和HRMS确证。分别采用MTT法和小鼠巨噬细胞Raw264.7炎症模型对目标化合物的体外细胞毒活性和抗炎活性进行测试,结果表明,哌嗪环上的取代基对化合物的生物活性有明显的影响。特别是化合物3j和3k对肿瘤细胞株Hela和A549均表现出良好的体外抑制活性,而且化合物3d能有效抑制NO的生成,值得进一步研究。
In order to find new potent biological agents, twelve 4＇-（N-substitued-l-piperazinyl） furanyl chalcone derivatives （3a - 31） are designed and synthesized by the general principle of molecular hybridization. The structures are characterized by ^1 H NMR, ^13C NMR and HRMS. In vitro cytotoxic activities against a panel of human tumor cell lines （Hela, A549 and SGC7901 ） are tested by the MTT assay, and the anti-inflammatory activities in lipopolysaccharide （LPS）-stimulated RAW-264. 7 macrophages are evaluated. The result indicate that the substituents of the NH group of piperazine ring have an obvious influence on biological activities. Especially, compounds 3j and 3k are found to be the potent compounds against Hela and A549, and compounds 3d has inhibitory effect on the generation of NO, which can be taken as lead compounds for further SAR research.
出处
《化学通报》
CAS
CSCD
北大核心
2018年第1期77-82,共6页
Chemistry
基金
国家自然科学基金项目(81560620)
云南省科学技术厅-云南中医学院应用基础研究联合专项(2017FF117(-023))资助
关键词
呋喃查尔酮
合成
生物活性评价
Furanyl chalcone, Synthesis, Biological evaluation
