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Artemisinin-derived hybrids and their anticancer activity.
European Journal of Medicinal Chemistry ( IF 6.7 ) Pub Date : 2020-01-08 , DOI: 10.1016/j.ejmech.2020.112044
Feng Gao 1 , Zhou Sun 1 , Fangong Kong 1 , Jiaqi Xiao 1
Affiliation  

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.

中文翻译:

青蒿素衍生的杂种及其抗癌活性。

耐药性的出现和抗癌药物的低特异性是癌症治疗的主要挑战,并且会导致许多副作用,迫切需要开发新型抗癌药物。青蒿素衍生的化合物,带有含有过氧化物的倍半萜内酯部分,可以形成具有高反应性的自由基,除了典型的抗疟活性外,还具有多种药物特性,包括体外和体内抗癌活性。杂交分子具有提高特异性和克服耐药性的潜力,因此青蒿素骨架与其他抗癌药效团的杂交可能提供具有高特异性和抗耐药性癌症强大效力的新型抗癌候选物。
更新日期:2020-01-08
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