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Updated: Sep 25, 2025

Preparation of Stable Bicyclic Aziridinium Ions and Their Ring-Opening for the Synthesis of Azaheterocycles
Published on: August 22, 2018
Synthesis and biological evaluation of novel artemisone-piperazine-tetronamide hybrids
Meng-Xue Wei1, Jia-Ying Yu1, Xin-Xin Liu1
1State Key Laboratory of High-efficiency Utilization of Coal and Green Chemical Engineering, Ningxia Engineering Research Center for Natural Medicine, National Demonstration Center for Experimental Chemistry Education, College of Chemistry and Chemical Engineering, Ningxia University 489 Helanshan West Road Yinchuan 750021 China lixq@nxu.edu.cn.
Abstract:
For the first time, six novel artemisone-piperazine-tetronamide hybrids (12a-f) were efficiently synthesised from dihydroartemisinin (DHA) and investigated for their in vitro cytotoxicity against some human cancer cells and benign cells. All the targets showed good cytotoxic activity in vitro. Hybrid 12a exhibited much better inhibitory activity against human liver cancer cell line SMMC-7721 (IC50 = 0.03 ± 0.04 μM for 24 h) than the parent DHA (IC50 > 0.7 μM), and two references, vincristine (VCR; IC50 = 0.27 ± 0.03 μM) & cytosine arabinoside (ARA; IC50 = 0.63 ± 0.04 μM). Furthermore, hybrid 12a had low toxicity against human benign liver cell line LO2 (IC50 = 0.70 ± 0.02 μM for 24 h) compared with VCR, ARA, and DHA in vitro. Moreover, the inhibitory activity of hybrid 12a was obviously enhanced when human liver cancer cell line MHCC97H absorbed Fe2+ in vitro.
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