Synthesis and biological evaluation of novel artemisone-piperazine-tetronamide hybrids
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 . Hy...
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| Veröffentlicht in: | RSC advances 2021-05, Vol.11 (3), p.18333-18341 |
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| container_title | RSC advances |
| container_volume | 11 |
| creator | Wei, Meng-Xue Yu, Jia-Ying Liu, Xin-Xin Li, Xue-Qiang Yang, Jin-Hui Zhang, Meng-Wei Yang, Pei-Wen Zhang, Si-Si He, Yu |
| description | 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 (IC
50
= 0.03 ± 0.04 μM for 24 h) than the parent DHA (IC
50
> 0.7 μM), and two references, vincristine (VCR; IC
50
= 0.27 ± 0.03 μM) & cytosine arabinoside (ARA; IC
50
= 0.63 ± 0.04 μM). Furthermore, hybrid
12a
had low toxicity against human benign liver cell line LO2 (IC
50
= 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 Fe
2+
in vitro
.
Six novel artemisone-piperazine-tetronamide hybrids were efficiently synthesised and investigated for their cytotoxicity against some human cancer cells. |
| doi_str_mv | 10.1039/d1ra00750e |
| format | Article |
| fullrecord | <record><control><sourceid>proquest_pubme</sourceid><recordid>TN_cdi_pubmedcentral_primary_oai_pubmedcentral_nih_gov_9033422</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>2531551914</sourcerecordid><originalsourceid>FETCH-LOGICAL-c428t-27a5748c640fd1c24b5be8d3f8a1e536625d9cdf1a248bde52453caaeb37af443</originalsourceid><addsrcrecordid>eNpdkc1LHEEQxZugRFEvuUcGchFhTH_PzCUgxi8QhHxdm5ruGrdltnvtnlnY_PWOrtmodamC-vF4j0fIJ0ZPGBXNV8cSUFopih_ILqdSl5zqZuvVvUMOcr6n02jFuGYfyY5QsqYNZ7vkz89VGGaYfS4guKL1sY933kJf4BL6EQYfQxG7IsQl9gWkAec-x4Dlwi8wwV8_nQMOKQaYe4fFbNUm7_I-2e6gz3jwsvfI74vzX2dX5c3t5fXZ6U1pJa-HklegKllbLWnnmOWyVS3WTnQ1MFRCa65cY13HgMu6dai4VMICYCsq6KQUe-TbWncxtnN0FsOQoDeL5OeQViaCN28_wc_MXVyahgohOZ8Ejl4EUnwYMQ9mymex7yFgHLPhWulKVlTWE_rlHXofxxSmeIYrwZRiDXtydLymbIo5J-w2Zhg1T42Z7-zH6XNj5xN8-Nr-Bv3XzwR8XgMp2833f-XiEZ6tnNs</addsrcrecordid><sourcetype>Open Access Repository</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype><pqid>2531551914</pqid></control><display><type>article</type><title>Synthesis and biological evaluation of novel artemisone-piperazine-tetronamide hybrids</title><source>DOAJ Directory of Open Access Journals</source><source>Elektronische Zeitschriftenbibliothek - Frei zugängliche E-Journals</source><source>PubMed Central Open Access</source><source>PubMed Central</source><creator>Wei, Meng-Xue ; Yu, Jia-Ying ; Liu, Xin-Xin ; Li, Xue-Qiang ; Yang, Jin-Hui ; Zhang, Meng-Wei ; Yang, Pei-Wen ; Zhang, Si-Si ; He, Yu</creator><creatorcontrib>Wei, Meng-Xue ; Yu, Jia-Ying ; Liu, Xin-Xin ; Li, Xue-Qiang ; Yang, Jin-Hui ; Zhang, Meng-Wei ; Yang, Pei-Wen ; Zhang, Si-Si ; He, Yu</creatorcontrib><description>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 (IC
50
= 0.03 ± 0.04 μM for 24 h) than the parent DHA (IC
50
> 0.7 μM), and two references, vincristine (VCR; IC
50
= 0.27 ± 0.03 μM) & cytosine arabinoside (ARA; IC
50
= 0.63 ± 0.04 μM). Furthermore, hybrid
12a
had low toxicity against human benign liver cell line LO2 (IC
50
= 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 Fe
2+
in vitro
.
Six novel artemisone-piperazine-tetronamide hybrids were efficiently synthesised and investigated for their cytotoxicity against some human cancer cells.</description><identifier>ISSN: 2046-2069</identifier><identifier>EISSN: 2046-2069</identifier><identifier>DOI: 10.1039/d1ra00750e</identifier><identifier>PMID: 35480921</identifier><language>eng</language><publisher>England: Royal Society of Chemistry</publisher><subject>Biotechnology ; Chemistry ; Liver cancer ; Toxicity</subject><ispartof>RSC advances, 2021-05, Vol.11 (3), p.18333-18341</ispartof><rights>This journal is © The Royal Society of Chemistry.</rights><rights>Copyright Royal Society of Chemistry 2021</rights><rights>This journal is © The Royal Society of Chemistry 2021 The Royal Society of Chemistry</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c428t-27a5748c640fd1c24b5be8d3f8a1e536625d9cdf1a248bde52453caaeb37af443</citedby><cites>FETCH-LOGICAL-c428t-27a5748c640fd1c24b5be8d3f8a1e536625d9cdf1a248bde52453caaeb37af443</cites><orcidid>0000-0002-8706-911X</orcidid></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC9033422/pdf/$$EPDF$$P50$$Gpubmedcentral$$Hfree_for_read</linktopdf><linktohtml>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC9033422/$$EHTML$$P50$$Gpubmedcentral$$Hfree_for_read</linktohtml><link.rule.ids>230,314,727,780,784,864,885,27924,27925,53791,53793</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/35480921$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Wei, Meng-Xue</creatorcontrib><creatorcontrib>Yu, Jia-Ying</creatorcontrib><creatorcontrib>Liu, Xin-Xin</creatorcontrib><creatorcontrib>Li, Xue-Qiang</creatorcontrib><creatorcontrib>Yang, Jin-Hui</creatorcontrib><creatorcontrib>Zhang, Meng-Wei</creatorcontrib><creatorcontrib>Yang, Pei-Wen</creatorcontrib><creatorcontrib>Zhang, Si-Si</creatorcontrib><creatorcontrib>He, Yu</creatorcontrib><title>Synthesis and biological evaluation of novel artemisone-piperazine-tetronamide hybrids</title><title>RSC advances</title><addtitle>RSC Adv</addtitle><description>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 (IC
50
= 0.03 ± 0.04 μM for 24 h) than the parent DHA (IC
50
> 0.7 μM), and two references, vincristine (VCR; IC
50
= 0.27 ± 0.03 μM) & cytosine arabinoside (ARA; IC
50
= 0.63 ± 0.04 μM). Furthermore, hybrid
12a
had low toxicity against human benign liver cell line LO2 (IC
50
= 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 Fe
2+
in vitro
.
Six novel artemisone-piperazine-tetronamide hybrids were efficiently synthesised and investigated for their cytotoxicity against some human cancer cells.</description><subject>Biotechnology</subject><subject>Chemistry</subject><subject>Liver cancer</subject><subject>Toxicity</subject><issn>2046-2069</issn><issn>2046-2069</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2021</creationdate><recordtype>article</recordtype><recordid>eNpdkc1LHEEQxZugRFEvuUcGchFhTH_PzCUgxi8QhHxdm5ruGrdltnvtnlnY_PWOrtmodamC-vF4j0fIJ0ZPGBXNV8cSUFopih_ILqdSl5zqZuvVvUMOcr6n02jFuGYfyY5QsqYNZ7vkz89VGGaYfS4guKL1sY933kJf4BL6EQYfQxG7IsQl9gWkAec-x4Dlwi8wwV8_nQMOKQaYe4fFbNUm7_I-2e6gz3jwsvfI74vzX2dX5c3t5fXZ6U1pJa-HklegKllbLWnnmOWyVS3WTnQ1MFRCa65cY13HgMu6dai4VMICYCsq6KQUe-TbWncxtnN0FsOQoDeL5OeQViaCN28_wc_MXVyahgohOZ8Ejl4EUnwYMQ9mymex7yFgHLPhWulKVlTWE_rlHXofxxSmeIYrwZRiDXtydLymbIo5J-w2Zhg1T42Z7-zH6XNj5xN8-Nr-Bv3XzwR8XgMp2833f-XiEZ6tnNs</recordid><startdate>20210521</startdate><enddate>20210521</enddate><creator>Wei, Meng-Xue</creator><creator>Yu, Jia-Ying</creator><creator>Liu, Xin-Xin</creator><creator>Li, Xue-Qiang</creator><creator>Yang, Jin-Hui</creator><creator>Zhang, Meng-Wei</creator><creator>Yang, Pei-Wen</creator><creator>Zhang, Si-Si</creator><creator>He, Yu</creator><general>Royal Society of Chemistry</general><general>The Royal Society of Chemistry</general><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7SR</scope><scope>8BQ</scope><scope>8FD</scope><scope>JG9</scope><scope>7X8</scope><scope>5PM</scope><orcidid>https://orcid.org/0000-0002-8706-911X</orcidid></search><sort><creationdate>20210521</creationdate><title>Synthesis and biological evaluation of novel artemisone-piperazine-tetronamide hybrids</title><author>Wei, Meng-Xue ; Yu, Jia-Ying ; Liu, Xin-Xin ; Li, Xue-Qiang ; Yang, Jin-Hui ; Zhang, Meng-Wei ; Yang, Pei-Wen ; Zhang, Si-Si ; He, Yu</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c428t-27a5748c640fd1c24b5be8d3f8a1e536625d9cdf1a248bde52453caaeb37af443</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2021</creationdate><topic>Biotechnology</topic><topic>Chemistry</topic><topic>Liver cancer</topic><topic>Toxicity</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Wei, Meng-Xue</creatorcontrib><creatorcontrib>Yu, Jia-Ying</creatorcontrib><creatorcontrib>Liu, Xin-Xin</creatorcontrib><creatorcontrib>Li, Xue-Qiang</creatorcontrib><creatorcontrib>Yang, Jin-Hui</creatorcontrib><creatorcontrib>Zhang, Meng-Wei</creatorcontrib><creatorcontrib>Yang, Pei-Wen</creatorcontrib><creatorcontrib>Zhang, Si-Si</creatorcontrib><creatorcontrib>He, Yu</creatorcontrib><collection>PubMed</collection><collection>CrossRef</collection><collection>Engineered Materials Abstracts</collection><collection>METADEX</collection><collection>Technology Research Database</collection><collection>Materials Research Database</collection><collection>MEDLINE - Academic</collection><collection>PubMed Central (Full Participant titles)</collection><jtitle>RSC advances</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Wei, Meng-Xue</au><au>Yu, Jia-Ying</au><au>Liu, Xin-Xin</au><au>Li, Xue-Qiang</au><au>Yang, Jin-Hui</au><au>Zhang, Meng-Wei</au><au>Yang, Pei-Wen</au><au>Zhang, Si-Si</au><au>He, Yu</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Synthesis and biological evaluation of novel artemisone-piperazine-tetronamide hybrids</atitle><jtitle>RSC advances</jtitle><addtitle>RSC Adv</addtitle><date>2021-05-21</date><risdate>2021</risdate><volume>11</volume><issue>3</issue><spage>18333</spage><epage>18341</epage><pages>18333-18341</pages><issn>2046-2069</issn><eissn>2046-2069</eissn><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 (IC
50
= 0.03 ± 0.04 μM for 24 h) than the parent DHA (IC
50
> 0.7 μM), and two references, vincristine (VCR; IC
50
= 0.27 ± 0.03 μM) & cytosine arabinoside (ARA; IC
50
= 0.63 ± 0.04 μM). Furthermore, hybrid
12a
had low toxicity against human benign liver cell line LO2 (IC
50
= 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 Fe
2+
in vitro
.
Six novel artemisone-piperazine-tetronamide hybrids were efficiently synthesised and investigated for their cytotoxicity against some human cancer cells.</abstract><cop>England</cop><pub>Royal Society of Chemistry</pub><pmid>35480921</pmid><doi>10.1039/d1ra00750e</doi><tpages>9</tpages><orcidid>https://orcid.org/0000-0002-8706-911X</orcidid><oa>free_for_read</oa></addata></record> |
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| language | eng |
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| source | DOAJ Directory of Open Access Journals; Elektronische Zeitschriftenbibliothek - Frei zugängliche E-Journals; PubMed Central Open Access; PubMed Central |
| subjects | Biotechnology Chemistry Liver cancer Toxicity |
| title | Synthesis and biological evaluation of novel artemisone-piperazine-tetronamide hybrids |
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