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《天津医科大学学报》[ISSN:1006-8147/CN:12-1259/R]

卷:

22卷

期数:

2016年03期

页码:

191-194

栏目:

基础医学

出版日期:

2016-05-20

文章信息/Info

Title:

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

文章编号:

1006-8147（2016）03-0191-04

作者:

?陈家浩¹; 方海军¹; 秦 楠¹; 2; 段宏泉¹; 2

(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)

Author(s):

CHEN Jia-hao¹;  FANG Hai-jun¹;  QIN Nan¹;  2; DUAN Hong-quan ¹;  2

(1.School of Pharmacy, Tianjin Medical University,Tianjin Key Laboratory on Technologies Enabling Development of Clinical Therapeutics and Diagnostics (Theranostics), Tianjin 300070, China; 2.Research Center of Basic Medical Sciences, Tianjin Medical University, Tianjin 300070, China)

关键词:

紫罗兰酮; 酰胺衍生物; 抗肿瘤转移

Keywords:

ionone; amide derivative;  anti-metastasis

分类号:

R9

DOI:

-

文献标志码:

A

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。

Abstract:

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 reactionfrom α-ionone as starting material. Results: Twelve ionone amide derivatives were synthesized by organic chemistry reactions. All of the compounds were identified by ¹H-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.

参考文献/References:

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备注/Memo

备注/Memo:

基金项目? 国家自然科学基金面上项目（81373297）

作者简介? 陈家浩（1989-），男，硕士在读，研究方向：天然产物结构改造；通信作者：段宏泉，E-mail:duanhq@tijmu.edu.cn。

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更新日期/Last Update: 2016-05-24