新型二硫醚蛇床子素衍生物的合成及抗增殖活性  

Synthesis and Antiproliferative Activity of Novel Dithioether Osthole Derivatives

作　　者：张汝国[1] 王小果[1] Zhang Ruguo;Wang Xiaoguo(Qiannan Medical College for Nationalities,Duyun 558000,China)

机构地区：[1]黔南民族医学高等专科学校,贵州都匀558000

出　　处：《广东化工》2023年第10期38-40,共3页Guangdong Chemical Industry

基　　金：黔南民族医学高等专科学校基金资助项目(QNYZ201839)。

摘　　要：为寻找高效低毒的抗肿瘤先导化合物,依据药物分子设计中的拼合原理,设计合成系列含二硫醚单元的蛇床子素衍生物,利用核磁共振氢谱和碳谱对其结构及性质进行表征和分析。采用MTT法对目标化合物进行体外抗肿瘤活性测试,结果显示目标化合物对各肿瘤细胞均具有一定的抑制活性。其中,对MCF-7细胞最为敏感,化合物的IC50值在10.8~17.1μmol·L^(-1)之间,其中5a的IC_(50)为10.8μmol·L^(-1),强于氟脲嘧啶(20.8μmol·L^(-1))和顺铂(13.9μmol·L^(-1))。初步构效关系表明,目标化合物对各肿瘤细胞增殖的抑制活性随着R直链烷烃上碳原子的增多而逐渐降低,当R为甲基时,目标化合物的抗增殖活性显著提高。For the aim of exploring new anti-tumor leading compounds with high efficiency and low toxicity,a series of osthole derivatives containing disulfide units were designed and synthesized according to the splicing principle in drug design.The structures of compounds were characterized by 1H NMR and 13C NMR.The in vitro antitumor activity of the target compounds was tested by MTT method,and the results showed that the target compound had a certain inhibitory activity on each tumor cell.It is the most sensitive to MCF-7 cells,and the IC_(50 )values of compounds are between 10.8 and 17.1μmol·L^(-1).Among them,the IC50 of 5a is 10.8μmol·L^(-1),which is stronger than that of fluorouracil(20.8μmol·L^(-1))and cisplatin(13.9μmol·L^(-1)).The preliminary structure-activity relationship showed that the inhibitory activity of the target compounds on the proliferation of tumor cells gradually decreased with the increase of carbon atoms on R straight chain alkanes.

关 键 词：二硫醚衍生物 蛇床子素 抗增殖活性 合成 

分 类 号：TQ465.91[化学工程—制药化工]