紫罗兰酮酰胺衍生物的合成与抗肿瘤转移活性研究  

Study on the ionone amide derivatives synthesis and anti-tumor metastatic effect

作　　者：陈家浩[1] 方海军[1] 秦楠[1,2] 段宏泉[1,2] 

机构地区：[1]天津医科大学药学院天津市临床药物关键技术重点实验室,天津300070 [2]天津医科大学基础医学研究中心,天津300070

出　　处：《天津医科大学学报》2016年第3期191-194,共4页Journal of Tianjin Medical University

基　　金：国家自然科学基金面上项目基金资助(81373297)

摘　　要：目的:研究紫罗兰酮酰胺衍生物的合成与抗肿瘤转移活性。方法:以α-紫罗兰酮为原料,经卤仿反应、烯丙位氧化反应和酰胺化反应得到目标化合物2a-f和4a-f,所有衍生物均评价其抗肿瘤转移活性。结果:合成得到两个系列共12个紫罗兰酮酰胺衍生物,所有化合物都经过1H NMR、13C NMR和ESI-MS表征了化学结构。与阳性对照化合物LY204002相比,化合物4f具有较强的抗肿瘤转移的活性。结论:紫罗兰酮酰胺衍生物中叔胺基团和3位羰基很可能是发挥抗肿瘤转移作用的必需基团。Objective： To study the ionone amide derivatives synthesis and anti-metastatic activities. Methods： Target compounds 2a-f and 4a-f were prepared by haloform reaction, allylic oxidation, amidation reaction from α-ionone as starting material. Results： Twelve ionone amide derivatives were synthesized by organic chemistry reactions. All of the compounds were identified by1H-NMR,13C-NMR and ESI-MS. Compared to the positive control compound LY294002, these results showed that compound 4f had significant anti-metastasis effect. Conclusion： The tertiary amine group and carbonyl group at C-3 position of ionone amide derivatives may be the essential in the anti-tumor metastasis.

关 键 词：紫罗兰酮 酰胺衍生物 抗肿瘤转移 

分 类 号：R9[医药卫生—药学]