兰州大学机构库 >药学院
Design, synthesis and antineoplastic activity of novel 20(S)-acylthiourea derivatives of camptothecin
Yang, Cheng-Jie1; Li, Bin4; Zhang, Zhi-Jun1; Gao, Jian-Mei1; Wang, Mei-Juan1; Zhao, Xiao-Bo1; Song, Zi-Long1; Liu, YQ(刘映前)1,2; Li, Hu1; Chen, Yuyuan4; Lee, Kuo-Hsiung3; Morris-Natschke, Susan L.3; Xu, Chuanrui4
2020-02
Source PublicationEUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
ISSN0223-5234
Volume187
AbstractFor the purpose of advancing our research on diverse C-20 decorated derivatives of camptothecin (CPT), 46 new CPT acylthiourea derivatives were synthesized and evaluated in vitro for their cytotoxicity. All the compounds showed promising in vitro cytotoxicity against six tumor cell lines (Hep3B, MCF7, A549, MDA-MB-231, KB and KB-vin). Out of them, compound c20 possesses remarkable in vitro cytotoxic activity and is more potent than topotecan. Mechanistically, c20 not only induces cell cycle arrest and cell apoptosis in A549 cells, but also inhibits Topo 1 activity in the cell and cell-free system in a manner similar to that of topotecan. In both xenograft and primary HCC mouse models, c20 displays significant in vivo anti-cancer activity and is more potent than topotecan. In addition, the acute toxicity assay showed that c20 has no apparent toxicity to mouse liver, kidney and hemopoietic system of the FVB/N mice. Take together, these results indicated that compound c20 could be a potential anti-cancer candidate for further clinical trial. (C) 2019 Elsevier Masson SAS. All rights reserved.
KeywordCamptothecin Acylthioureas Topoisomerase I Cytotoxicity
DOI10.1016/j.ejmech.2019.111971
Indexed BySCIE ; IC
Language英语
Funding ProjectNational Natural Science Foundation of China[21672092][21877056][81572723] ; Key Program for international S&T cooperation projects of China Gansu Province[18YF1WA115] ; Opening Project of Zhejiang Provincial Preponderant and Characteristic Subject of Key University (Traditional Chinese Pharmacology), Zhejiang Chinese Medical University[ZYA0X2018009] ; Innovation Foundation of Higher Education of China[2016JCTD109][0118650030] ; Fundamental Research Funds for the Central Universities[lzujbky-2016-147][lzujbky-2017-k23]
WOS Research AreaPharmacology & Pharmacy
WOS SubjectChemistry, Medicinal
WOS IDWOS:000510525000050
PublisherELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
Original Document TypeArticle
Citation statistics
Cited Times:0[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Identifierhttp://ir.lzu.edu.cn/handle/262010/417782
Collection药学院
Corresponding AuthorLiu, Ying-Qian; Xu, Chuanrui
Affiliation1.Lanzhou Univ, Sch Pharm, Lanzhou 730000, Peoples R China
2.Zhejiang Chinese Med Univ, Coll Pharmaceut Sci, Hangzhou 310000, Peoples R China
3.Univ N Carolina, UNC Eshelman Sch Pharm, Nat Prod Res Labs, Chapel Hill, NC 27599 USA
4.Huazhong Univ Sci & Technol, Tongji Med Coll, Sch Pharm, Wuhan 430030, Peoples R China
First Author AffilicationSchool of Pharmacy
Corresponding Author AffilicationSchool of Pharmacy
Recommended Citation
GB/T 7714
Yang, Cheng-Jie,Li, Bin,Zhang, Zhi-Jun,et al. Design, synthesis and antineoplastic activity of novel 20(S)-acylthiourea derivatives of camptothecin[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2020,187.
APA Yang, Cheng-Jie.,Li, Bin.,Zhang, Zhi-Jun.,Gao, Jian-Mei.,Wang, Mei-Juan.,...&Xu, Chuanrui.(2020).Design, synthesis and antineoplastic activity of novel 20(S)-acylthiourea derivatives of camptothecin.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,187.
MLA Yang, Cheng-Jie,et al."Design, synthesis and antineoplastic activity of novel 20(S)-acylthiourea derivatives of camptothecin".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 187(2020).
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