{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Wei MX"],"funding":["Natural Science Foundation of Ningxia Province","National Natural Science Foundation of China","Ningxia University"],"pagination":["18333-18341"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC9033422"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["11(30)"],"pubmed_abstract":["For the first time, six novel artemisone-piperazine-tetronamide hybrids (12a-f) were efficiently synthesised from dihydroartemisinin (DHA) and investigated for their <i>in vitro</i> cytotoxicity against some human cancer cells and benign cells. All the targets showed good cytotoxic activity <i>in vitro</i>. Hybrid 12a exhibited much better inhibitory activity against human liver cancer cell line SMMC-7721 (IC<sub>50</sub> = 0.03 ± 0.04 μM for 24 h) than the parent DHA (IC<sub>50</sub> > 0.7 μM), and two references, vincristine (VCR; IC<sub>50</sub> = 0.27 ± 0.03 μM) & cytosine arabinoside (ARA; IC<sub>50</sub> = 0.63 ± 0.04 μM). Furthermore, hybrid 12a had low toxicity against human benign liver cell line LO2 (IC<sub>50</sub> = 0.70 ± 0.02 μM for 24 h) compared with VCR, ARA, and DHA <i>in vitro</i>. Moreover, the inhibitory activity of hybrid 12a was obviously enhanced when human liver cancer cell line MHCC97H absorbed Fe<sup>2+</sup> <i>in vitro</i>."],"journal":["RSC advances"],"pubmed_title":["Synthesis and biological evaluation of novel artemisone-piperazine-tetronamide hybrids."],"pmcid":["PMC9033422"],"funding_grant_id":["21462032","2021AAC05009","2019AAC03018","G2020107490003"],"pubmed_authors":["Zhang SS","Li XQ","Yang JH","He Y","Wei MX","Liu XX","Yu JY","Yang PW","Zhang MW"],"additional_accession":[]},"is_claimable":false,"name":"Synthesis and biological evaluation of novel artemisone-piperazine-tetronamide hybrids.","description":"For the first time, six novel artemisone-piperazine-tetronamide hybrids (12a-f) were efficiently synthesised from dihydroartemisinin (DHA) and investigated for their <i>in vitro</i> cytotoxicity against some human cancer cells and benign cells. All the targets showed good cytotoxic activity <i>in vitro</i>. Hybrid 12a exhibited much better inhibitory activity against human liver cancer cell line SMMC-7721 (IC<sub>50</sub> = 0.03 ± 0.04 μM for 24 h) than the parent DHA (IC<sub>50</sub> > 0.7 μM), and two references, vincristine (VCR; IC<sub>50</sub> = 0.27 ± 0.03 μM) & cytosine arabinoside (ARA; IC<sub>50</sub> = 0.63 ± 0.04 μM). Furthermore, hybrid 12a had low toxicity against human benign liver cell line LO2 (IC<sub>50</sub> = 0.70 ± 0.02 μM for 24 h) compared with VCR, ARA, and DHA <i>in vitro</i>. Moreover, the inhibitory activity of hybrid 12a was obviously enhanced when human liver cancer cell line MHCC97H absorbed Fe<sup>2+</sup> <i>in vitro</i>.","dates":{"release":"2021-01-01T00:00:00Z","publication":"2021 May","modification":"2025-04-05T20:04:24.245Z","creation":"2025-04-05T20:04:24.245Z"},"accession":"S-EPMC9033422","cross_references":{"pubmed":["35480921"],"doi":["10.1039/d1ra00750e"]}}