Novel derivatives bearing a ferrocene attached via a piperazine linker to C-10 of the artemisinin nucleus were prepared from dihydroartemisinin and screened against chloroquine (CQ) sensitive NF54 and CQ resistant K1 and W2 strains of Plasmodium falciparum (Pf) parasites. The overall aim is to imprint oxidant (from the artemisinin) and redox (from the ferrocene) activities. In a preliminary assessment, these compounds were shown to possess activities in the low nM range with the most active being compound 6 with IC₅₀ values of 2.79 nM against Pf K1 and 3.2 nM against Pf W2. Overall the resistance indices indicate that the compounds have a low potential for cross resistance. Cytotoxicities were determined with Hek293 human embryonic kidney cells and activities against proliferating cells were assessed against A375 human malignant melanoma cells. The selectivity indices of the amino-artemisinin ferrocene derivatives indicate there is overall an appreciably higher selectivity towards the malaria parasite than mammalian cells.

从双氢青蒿素制备了通过哌嗪连接体连接到青蒿素核 C-10 上的二茂铁的新型衍生物，并针对氯喹 (CQ) 敏感的 NF54 和 CQ 抗性 K1 和 W2 菌株恶性疟原虫( Pf ) 寄生虫进行筛选。总体目标是印记氧化剂（来自青蒿素）和氧化还原（来自二茂铁）活性。在初步评估，被证明这些化合物具有在低nM范围的活动最活跃的存在化合物6与IC _50个2.79纳米的对值Pf的K1和3.2 nM的针对Pf的W2。总体而言，抗性指数表明这些化合物具有低的交叉抗性潜力。用 Hek293 人胚胎肾细胞测定细胞毒性，并针对 A375 人恶性黑色素瘤细胞评估对增殖细胞的活性。氨基青蒿素二茂铁衍生物的选择性指数表明总体上对疟原虫的选择性比哺乳动物细胞高得多。