期刊论文

Liu Jianchao

中文

有机化学

0253-2786

2015

35

2

462-466

10.6023/cjoc201408036

National Program on Key Basic Research Project (973 Program)National Basic Research Program of China [2010CB126100]; National Natural Science Foundation of ChinaNational Natural Science Foundation of China (NSFC) [21172090, 31000867]; Program for Changjiang Scholars and Innovatives Research Team in UniversityProgram for Changjiang Scholars & Innovative Research Team in University (PCSIRT) [IRT0953]

本校为第一且通讯机构

利用生物活性亚结构拼接原理, 将活性酰腙亚结构与活性噻唑环亚结构进行拼接, 设计合成了14个新型N'-芳基亚甲基-N-(4-取代苯甲酰氧基噻唑-2-基)取代苯甲酰腙衍生物.所有目标化合物经~1H NMR、IR、质谱及元素分析等手段进行了表征, 部分化合物还经过~(13)C NMR进行了确证. 抗肿瘤测试结果表明, 该系列化合物表现出明显的抗肿瘤活性, 其对人口腔上皮癌细胞株(KB)的抑制活性优于对鼻咽癌细胞株(CNE2)的抑制活性; 采用离体平皿法对目标化合物进行杀菌活性测试, 测试菌种为: 小麦赤霉菌、水稻纹枯霉菌、黄瓜灰霉菌、番茄早疫菌、烟草赤星菌和黄瓜炭疽菌. 结果表明, 在1.0×10~(-4)g/mL浓度下, 目标化...

14 novel N'-arylmethylene-N-(4-benzoyloxy-thiazole-2-yl) benzoylhydrazone derivatives were designed and synthesized by incorporating the activated structural templets of thiazole and acylhydrazone. All the target compounds were characterized by 1H NMR, IR, mass spectrometry and elemental analysis, and some of the compounds were confirmed by 13C NMR. Anti-tumor test results showed that the hydrazone compounds showed significant anti-tumor activity. These compounds were more active against the KB cell lines than the CNE2 cell lines. All synthesiz...