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ID: ALA4732241
Journal: Eur J Med Chem
Title: Synthesis of artemisinin-piperazine-furan ether hybrids and evaluation of in vitro cytotoxic activity.
Authors: Wei MX,Yu JY,Liu XX,Li XQ,Zhang MW,Yang PW,Yang JH
Abstract: For the first time, eight novel artemisinin-piperazine-furane ether hybrids (5a-h) were efficiently synthesized and investigated for their in vitro cytotoxic activity against some human cancer and benign cells. The absolute configuration of hybrid 5c was determined by X-ray crystallographic analysis. Hybrids 5a-h exhibited more pronounced growth-inhibiting action on hepatocarcinoma cell lines than their parent dihydroartemisinin (DHA) and the reference cytosine arabinoside (ARA). The hybrid 5a showed the best cytotoxic activity against human hepatocarcinoma cells SMMC-7721 (IC = 0.26 ± 0.03 μM) after 24 h. Furthermore, hybrid 5a also showed good cytotoxic activity against human breast cancer cells MCF-7 and low cytotoxicity against human breast benign cells MCF-10A in vitro. We found the cytotoxicity of hybrid 5a did not change when tumour cells absorb iron sulfate (FeSO); thus, we conclude the anti-tumour mechanism induced by iron ions (Fe) is unclear.
CiteXplore: 33636536