β-榄香烯醇酯类化合物的合成及抗癌活性研究  

Synthesis and antitumor activity of β-elemene-13-yl esters

作　　者：张兴忠[1] 徐莉英[1] 陶淑娟[1] 王宪明[2] 陈光[2] 王敏伟[2] 董金华[1] 

机构地区：[1]沈阳药科大学制药工程学院,辽宁沈阳110016 [2]沈阳药科大学药学院,辽宁沈阳110016

出　　处：《中国药物化学杂志》2007年第1期13-17,共5页Chinese Journal of Medicinal Chemistry

基　　金：辽宁省教育厅高等学校科研基金项目(202043228)

摘　　要：目的设计合成β-榄香烯醇酯类化合物,并进行体外抗癌活性筛选。方法采用烯丙位的氯代反应,先合成β-榄香烯氯代物,再与羧酸或氨基酸反应合成目标化合物。用SRB法测定目标化合物对癌细胞的增殖抑制作用。结果共合成10个未见报道的β-榄香烯醇酯类化合物,其结构经红外光谱、核磁共振氢谱和质谱确证。所合成的多个化合物对3种人癌细胞HL-60、HeLa、SGC-7901的IC50值低于β-榄香烯。结论通过在β-榄香烯结构中引入含氮、含氧基团,改善其水溶性,可以提高体外抗癌活性。Aim To design and synthesize a series of β-elemene-13-yl esters, and to evaluate their antitumor activity in vitro. Methods The target compounds were synthesized from β-elemene via chlorination and nucleophilic substitution. Their effects on growth inhibition against HL-60, HeLa and SGC-7901 cells were determined by SRB assay. Results Ten compounds that had not been reported were synthesized and their structures were confirmed by IR, 1H-NMR and MS. Most of the synthesized compounds had higher antiproliferative activities than that of fl-elemene. Conclusion An introduction of carboxylic group and amino group into the skeleton of fl-elemene would increase its antitumor activity.

关 键 词：β-榄香烯衍生物 抗癌活性 SRB法 

分 类 号：R914[医药卫生—药物化学]