β-榄香烯酰亚胺类衍生物的合成及抗增殖作用研究  

Synthesis and anti-proliferative activity of theβ-elemene imide-containing derivatives

作　　者：刘德志 苏浩尘 邹越薪 景永奎[2] 徐莉英[1] 张美慧[1] 董金华[1] LIU De-zhi;SU Hao-chen;ZOU Yue-xin;JING Yong-kui;XU Li-ying;ZHANG Mei-hui;DONG Jin-hua(Key Laboratory of Structure-Based Drug Design&Discovery(Shenyang Pharmaceutical University),Ministry of Education,Shenyang 110016,China;Wuya College of Innovation,Shenyang Pharmaceutical University,Shenyang 110016,China)

机构地区：[1]沈阳药科大学基于靶点的药物设计与研究教育部重点实验室,辽宁沈阳110016 [2]沈阳药科大学无涯创新学院,辽宁沈阳110016

出　　处：《中国药物化学杂志》2022年第11期821-825,833,共6页Chinese Journal of Medicinal Chemistry

基　　金：沈阳药科大学创新创业训练计划项目(202110163022)。

摘　　要：目的 设计合成β-榄香烯酰亚胺类衍生物并进行体外抗肿瘤活性筛选。方法 由单氯代β-榄香烯为起始原料,与酰亚胺反应合成β-榄香烯酰亚胺类衍生物。采用磺酰罗丹明B法测定了目标化合物对人淋巴瘤(Raji)细胞株的增殖抑制作用。结果 合成了13个未见文献报道的β-榄香烯酰亚胺类衍生物,其结构经~1H-NMR、ESI-MS波谱分析确证。体外抗肿瘤活性实验结果显示,目标化合物的活性均高于β-榄香烯。结论 在β-榄香烯结构中引入酰亚胺结构片段有利于提高β-榄香烯的抗增殖作用。For increasing the antitumor activity ofβ-elemene,thirteenβ-elemene imide-containing derivatives were designed and synthesized from 13-choloro-β-elemene via nucleophilic substitution.The structures of the target compounds were confirmed by~1H-NMR and MS.The in vitro anti-proliferative effects of the target compounds on Raji cells were determined by SRB assay.Preliminary pharmacological results showed that most compounds possessed more potent anti-proliferative activity thanβ-elemene.

关 键 词：Β-榄香烯 β-榄香烯酰亚胺类衍生物 抗增殖活性 合成 

分 类 号：R914[医药卫生—药物化学]