摘要
以脱氢表雄酮为原料,经多步反应合成5个侧链具有不同吲哚结构的过氧化甾腙衍生物。所有合成化合物都通过MS、1HNMR和13CNMR进行结构表征。另外,分别选用人肝癌细胞(Hep G2)、人乳腺癌细胞(MCF-7)和人正常肾上皮细胞(293T)对化合物的抗增殖活性进行评价,结果表明,3β-羟基-5α,8α-过氧化雄甾-6-烯-17-(5-氟-吲哚)腙和3β-羟基-5α,8α-过氧化雄甾-6-烯-17-(5-氯-吲哚)腙对所测试的肿瘤细胞株具有显著的抑制活性。
Using dehydroepiandrosterone(DHEA) as staring material,five steroidal endoperoxide detivatives with different indolesidechain structures had been synthesized,and the structures were confirmed by MS,1 HNMR and13 CNMR. The antiproliferative activity was evaluated against human liver carcinoma cells(Hep G2),human breast cervical cancer cells(MCF-7) and normal kidney epithelial cells(293 T). The results showed that 5α,8α-epidioxy-17-(5-fluoro-indol-3-ylmethylene) hydrazonoandrostan-3β-ol and 5α,8α-epidioxy-17-(5-chloro-indol-3-ylmethylene) hydrazonoandrostan-3β-ol had significant inhibitory activity to the tested cancer cells.
作者
卜明
由丹
张嵩
陈哲
BU Ming;YOU Dan;ZHANG Song;CHEN Zhe(School of Pharmacy,Qiqihar Medical University,Qiqihar 161006,China;Basic Medical Science College,Qiqihar Medical University,Qiqihar 161006,China;Research Institute of Medicine&Pharmacy,Qiqihar Medical University,Qiqihar 161006,China;The First Hospital of Qiqihar,Qiqihar 161006,China)
出处
《化学试剂》
CAS
北大核心
2019年第3期220-223,共4页
Chemical Reagents
基金
齐齐哈尔市科学技术计划项目(SFGG-201771)
关键词
脱氢表雄酮
甾体
过氧化物
吲哚
抗肿瘤活性
dehydroepiandrosterone
sterol
endoperoxide
indole
antitumor activity
