摘要
根据药效团拼合原理,设计并合成了结构新颖的青蒿素-苯丁酸氮芥酯,其结构由1H NMR、13C NMR和HRMS-ESI表征确定。体外抗增殖测试显示,青蒿素-苯丁酸氮芥酯对人白血病细胞K562和人白血病耐阿霉素细胞K562/ADR均具有较强的抑制活性,IC50值分别为3.065±0.568和15.173±1.297μmol/L。流式细胞术结果表明,青蒿素-苯丁酸氮芥酯能够阻滞K562和K562/ADR的细胞周期,并诱导细胞凋亡。
Based on the principle of pharmacophore combination,a novel chlorambucil ester of artemisinin(3)was synthesized and identified by 1H NMR,13C NMR and HRMS-ESI.The data of antiproliferative activity in vitro showed that compound 3 exhibited potential anticancer activity against human leukemia K562 and human adriamycin-resistance leukemia K562/ADR cells with IC50 values of 3.065±0.568 and 15.173±1.297μmol/L,respectively.Moreover,flow cytometry indicated that compound 3 could significantly trigger cell cycle arrest and induce apoptosis of K562 and K562/ADR cells,respectively.
作者
王合珍
程敬东
徐应淑
白国辉
张磊
陈永正
Wang He-zhen;Cheng Jing-dong;Xu Ying-shu;Bai Guo-hui;Zhang Lei;Chen Yong-zheng(Key Laboratory of Biocatalysis&Chiral Drug Synthesis of Guizhou Province,Zunyi Medical University,Zunyi 563000;School of Pharmacy,Zunyi Medical University,Zunyi 563000;Key Laboratory of Oral Disease of Higher Schools in Guizhou Province,Zunyi Medical University,Zunyi 563000)
出处
《国外医药（抗生素分册）》
CAS
2021年第1期55-58,共4页
World Notes on Antibiotics
基金
贵州省科技厅基础研究基金项目(黔科合基础[2017]1219)。
关键词
青蒿素-苯丁酸氮芥酯
合成
抗肿瘤活性
chlorambucil ester of artemisinin
synthesis
antiproliferative activity
