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 | |
刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS |
2019-01-15 | |
卷号 | 29期号:2页码:234-237 |
关键词 | Biodnylated Camptothecin Derivatives Anticancer Activity Synthesis Click Chemistry Structure-activity Relationships (Sars) |
ISSN号 | 0960-894X |
英文摘要 | 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. |
资助项目 | Yunnan province[2015HB093] ; Yunnan province[2015FB168] ; National Key Research and Development Program of China[2017YFD0201402] |
语种 | 英语 |
内容类型 | 期刊论文 |
源URL | [http://ir.kib.ac.cn/handle/151853/64334] |
专题 | 昆明植物研究所_植物化学与西部植物资源持续利用国家重点实验室 |
通讯作者 | Jiang, Zi-Hua; Hu, Jiang-Miao |
作者单位 | 1.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 |
推荐引用方式 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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