兰州大学机构库 >药学院
Design and synthesis of novel 7-[(N-substituted-thioureidopiperazinyl)-methyl]-camptothecin derivatives as potential cytotoxic agents
Song, Zi-Long1; Yang, Guan-Zhou1; Li, Jun-Cai1; Liu, YQ(刘映前)1; Yang, Chen-Jie1; Goto, Masuo2; Zhang, Zhi-Jun1; Morris-Natschke, Susan L.2; Liu, Hua1; Lee, Kuo-Hsiung2,3
2020-07-17
Source PublicationNATURAL PRODUCT RESEARCH
ISSN1478-6419
Volume34Issue:14Pages:2022-2029
AbstractAs part of continuing our research on diverse C-7 derivatives of camptothecin (CPT), 16 CPT derivatives bearing piperazinyl-thiourea chemical scaffold and different substituent groups have been designed, synthesized and evaluatedin vitrofor cytotoxicity against five tumor cell lines (A-549, MDA-MB-231, MCF-7, KB and KBvin). As a result, all the synthesized compounds showed promising in vitro cytotoxic activity against the five tumor cell lines tested, and were more potent than irinotecan. Importantly, compounds13 g(IC50= 0.514 mu M) and13o(IC50= 0.275 mu M) possessed similar or better antiproliferative activity against the multidrug-resistant (MDR) KBvin subline than that of topotecan (IC50= 0.511 mu M) and merit further development as anticancer candidates for clinical trail. With these results in hand, we have a reason to conclude that incorporating piperazinyl-thiourea motifs into position-7 of camptothecin confers well cytotoxic activity against cancer cell lines, probably resulting in new anticancer drugs.
KeywordCamptothecin piperazinyl-thiourea cytotoxic activity synthesis
DOI10.1080/14786419.2019.1573231
Indexed BySCIE
Language英语
WOS Research AreaChemistry ; Pharmacology & Pharmacy
WOS SubjectChemistry, Applied ; Chemistry, Medicinal
WOS IDWOS:000547162000010
PublisherTAYLOR & FRANCIS LTD
Original Document TypeArticle
Citation statistics
Cited Times:1[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Identifierhttp://ir.lzu.edu.cn/handle/262010/421921
Collection药学院
Corresponding AuthorLiu, Ying-Qian; Zhang, Zhi-Jun; Lee, Kuo-Hsiung
Affiliation1.Lanzhou Univ, Sch Pharm, Lanzhou, Peoples R China
2.Univ N Carolina, UNC Eshelman Sch Pharm, Nat Prod Res Labs, Chapel Hill, NC 27515 USA
3.China Med Univ & Hosp, Chinese Med Res & Dev Ctr, Taichung, Taiwan
First Author AffilicationSchool of Pharmacy
Corresponding Author AffilicationSchool of Pharmacy
Recommended Citation
GB/T 7714
Song, Zi-Long,Yang, Guan-Zhou,Li, Jun-Cai,et al. Design and synthesis of novel 7-[(N-substituted-thioureidopiperazinyl)-methyl]-camptothecin derivatives as potential cytotoxic agents[J]. NATURAL PRODUCT RESEARCH,2020,34(14):2022-2029.
APA Song, Zi-Long.,Yang, Guan-Zhou.,Li, Jun-Cai.,Liu, Ying-Qian.,Yang, Chen-Jie.,...&Lee, Kuo-Hsiung.(2020).Design and synthesis of novel 7-[(N-substituted-thioureidopiperazinyl)-methyl]-camptothecin derivatives as potential cytotoxic agents.NATURAL PRODUCT RESEARCH,34(14),2022-2029.
MLA Song, Zi-Long,et al."Design and synthesis of novel 7-[(N-substituted-thioureidopiperazinyl)-methyl]-camptothecin derivatives as potential cytotoxic agents".NATURAL PRODUCT RESEARCH 34.14(2020):2022-2029.
Files in This Item:
There are no files associated with this item.
Related Services
Recommend this item
Bookmark
Usage statistics
Export to Endnote
Altmetrics Score
Google Scholar
Similar articles in Google Scholar
[Song, Zi-Long]'s Articles
[Yang, Guan-Zhou]'s Articles
[Li, Jun-Cai]'s Articles
Baidu academic
Similar articles in Baidu academic
[Song, Zi-Long]'s Articles
[Yang, Guan-Zhou]'s Articles
[Li, Jun-Cai]'s Articles
Bing Scholar
Similar articles in Bing Scholar
[Song, Zi-Long]'s Articles
[Yang, Guan-Zhou]'s Articles
[Li, Jun-Cai]'s Articles
Terms of Use
No data!
Social Bookmark/Share
No comment.
Items in the repository are protected by copyright, with all rights reserved, unless otherwise indicated.