Synthesis and antitumor activity of biotinylated camptothecin derivatives as potent cytotoxic agents
Zi, Cheng-Ting1,2,3; Yang, Liu2; Xu, Feng-Qing2; Dong, Fa-Wu2; Ma, Rui-Jing2; Li, Yan2; Zhou, Jun2; Ding, Zhong-Tao3; Jiang, Zi-Hua4; Hu, Jiang-Miao2
2019-01-15
Source PublicationBIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN0960-894X
Volume29Issue:2Pages:234-237
Abstract

A series of biotinylated camptothecin derivatives were designed and synthesized. The key to the synthesis was achieved by employing an esterification reaction and click chemistry. All of the new derivatives were tested for cytotoxicity against five human tumor cell lines, including HL-60, SMMC-7721, A-549, MCF-7, and SW480 with IC50 values ranging from 0.13 to 21.53 mu M. Most of the derivatives exhibited potent cytotoxicity, especially compound 17 (IC50 = 0.13-3.31 mu M) and compound 18 (IC50 = 0.23-1.48 mu M), which exhibited the highest potencies. The structure-activity relationships (SARs) of the biotinylated camptothecin derivatives were discussed for exploring novel anticancer agents.

KeywordBiodnylated Camptothecin Derivatives Anticancer Activity Synthesis Click Chemistry Structure-activity Relationships (Sars)
Indexed BySCI
Language英语
Document Type期刊论文
Identifierhttp://ir.kib.ac.cn/handle/151853/64335
Collection植物化学与西部植物资源持续利用国家重点实验室
Corresponding AuthorJiang, Zi-Hua; Hu, Jiang-Miao
Affiliation1.Yunnan Agr Univ, Coll Sci, Key Lab Pu Er Tea Sci, Minist Educ, Kunming 650201, Yunnan, Peoples R China
2.Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources West Ch, Kunming 650201, Yunnan, Peoples R China
3.Yunnan Univ, Sch Chem Sci & Technol, Key Lab Med Chem Nat Resource, Minist Educ, Kunming 650091, Yunnan, Peoples R China
4.Lakehead Univ, Dept Chem, 955 Oliver Rd, Thunder Bay, ON P7B 5E1, Canada
Recommended Citation
GB/T 7714
Zi, Cheng-Ting,Yang, Liu,Xu, Feng-Qing,et al. Synthesis and antitumor activity of biotinylated camptothecin derivatives as potent cytotoxic agents[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2019,29(2):234-237.
APA Zi, Cheng-Ting.,Yang, Liu.,Xu, Feng-Qing.,Dong, Fa-Wu.,Ma, Rui-Jing.,...&Hu, Jiang-Miao.(2019).Synthesis and antitumor activity of biotinylated camptothecin derivatives as potent cytotoxic agents.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,29(2),234-237.
MLA Zi, Cheng-Ting,et al."Synthesis and antitumor activity of biotinylated camptothecin derivatives as potent cytotoxic agents".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 29.2(2019):234-237.
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