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Artemisinin-derived dimers from a chemical perspective
Medicinal Research Reviews ( IF 13.3 ) Pub Date : 2021-06-11 , DOI: 10.1002/med.21814
Aysun Çapcı 1 , Lars Herrmann 1 , Halmuthur M Sampath Kumar 1, 2 , Tony Fröhlich 1 , Svetlana B Tsogoeva 1
Affiliation  

Considerable progress has been made with the rather recently developed dimer approach, which has already found applications in the development of new effective artemisinin-derived antimalarial, anticancer, and antiviral agents. One observation common to these potential applications is the significant (i.e., much more than double) improvement in activity of artemisinin based dimers, which are not toxic to normal cells and have fewer or less harmful side effects, with respect to monomers against parasites, cancer cells and viruses. Due to the high potential of the dimerization concept, many new artemisinin-derived dimer compounds and their biological activities have been recently reported. In this review an overview of the synthesis of dimer drug candidates based on the clinically used drug artemisinin and its semisynthetic derivatives is given. Besides the highlighting of biological activities of the selected dimers, the main focus is set on different synthetic approaches toward the dimers containing a broad variety of symmetric and nonsymmetric linking moieties.

中文翻译:

从化学角度看青蒿素二聚体

最近开发的二聚体方法取得了相当大的进展,该方法已在开发新的有效青蒿素衍生的抗疟药、抗癌药和抗病毒药中得到应用。这些潜在应用的共同观察结果是基于青蒿素的二聚体的活性显着提高(即,超过两倍),对于抗寄生虫、癌症的单体而言,这些二聚体对正常细胞没有毒性并且具有更少或更少的有害副作用细胞和病毒。由于二聚化概念的高潜力,最近报道了许多新的青蒿素衍生二聚体化合物及其生物活性。本综述概述了基于临床常用药物青蒿素及其半合成衍生物的二聚体候选药物的合成。
更新日期:2021-06-11
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