青蒿素
药效团
化学
倍半萜内酯
合理设计
药品
药理学
结构-活动关系
计算生物学
体内
体外
组合化学
倍半萜
生物化学
立体化学
纳米技术
恶性疟原虫
生物
生物技术
疟疾
材料科学
免疫学
作者
Feng Gao,Zhou Sun,Fangong Kong,Jiaqi Xiao
标识
DOI:10.1016/j.ejmech.2020.112044
摘要
The emergence of drug-resistance and the low specificity of anticancer agents are the major challenges in the treatment of cancer and can result in many side effects, creating an urgent demand to develop novel anticancer agents. Artemisinin-derived compounds, bearing a peroxide-containing sesquiterpene lactone moiety, could form free radicals with high reactivity and possess diverse pharmaceutical properties including in vitro and in vivo anticancer activity besides their typical antimalarial activity. Hybrid molecules have the potential to improve the specificity and overcome the drug resistance, therefore hybridization of artemisinin skeleton with other anticancer pharmacophores may provide novel anticancer candidates with high specificity and great potency against drug-resistant cancers. The review outlines the recent advances of artemisinin-derived hybrids as potential anticancer agents, and the structure-activity relationships are also discussed to provide an insight for rational designs of novel hybrids with high activity.
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