新型螺双环青蒿素类似物（青蒿素类似物）：合成与抗肿瘤活性
Novel spirobicyclic artemisinin analogues (artemalogues): Synthesis and antitumor activities.
作者信息
Liu Gang, Song Shanshan, Shu Shiqi, Miao Zehong, Zhang Ao, Ding Chunyong
机构信息
CAS Key Laboratory of Receptor Research, and Synthetic Organic & Medicinal Chemistry Laboratory, Shanghai Institute of Materia Medica (SIMM), Chinese Academy of Sciences, Shanghai 201203, China.
State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica (SIMM), Chinese Academy of Sciences, Shanghai 201203, China.
出版信息
Eur J Med Chem. 2015 Oct 20;103:17-28. doi: 10.1016/j.ejmech.2015.08.035. Epub 2015 Aug 18.
The sesquiterpene lactone framework of artemisinin was used as a drug repositioning prototype for the development of novel antitumor drugs. Several series of novel artemisinin analogues (artemalogues) were designed and synthesized through 1,3-dipolar cycloaddition of artemisitene with nitrile oxides or nitrones. The isoxazolidine-containing spirobicyclic artemalogue 11b turns out to be the most potent with low micromolar IC₅₀ values against all three tumor cells, which were at least 4- to 14-fold more potent than the parent artemisinin.
青蒿素的倍半萜内酯骨架被用作开发新型抗肿瘤药物的药物重定位原型。通过青蒿烯与腈氧化物或硝酮的1,3-偶极环加成反应，设计并合成了几个系列的新型青蒿素类似物（青蒿类似物）。含异恶唑烷的螺双环青蒿类似物11b被证明是最有效的，对所有三种肿瘤细胞的IC₅₀值为低微摩尔浓度，其效力比母体青蒿素至少高4至14倍。
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