Synthesis and antitumor activity of 10-arylcamptothecin derivatives
文献类型：期刊论文
| 作者 | Jiao, Yu2; Liu, Hongchun1 ; Geng, Meiyu1; Duan, Wenhu2
|
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 |
| 出版日期 | 2011-04-01 |
| 卷号 | 21期号:7页码:2071-2074 |
| 关键词 | Antitumor activity Camptothecin derivative Lactone stability Synthesis Topoisomerase I inhibitor |
| ISSN号 | 0960-894X |
| DOI | 10.1016/j.bmcl.2011.02.005 |
| 文献子类 | Article |
| 英文摘要 | A series of 10-arylcamptothecin derivatives was designed and synthesized. The key step of the synthesis was achieved by employing Suzuki cross-coupling chemistry. All of the new derivatives were tested for cytotoxicity against three human tumor cell lines, BEL-7402, A549, and HL-60; most of the derivatives exhibited potent cytotoxicity. The stability study showed that compound 30 was more stable than its lead compound 10-hydroxycamptothecin under the physiological condition. Mechanistic study demonstrated that compound 30 and its hydrochloride 31 had a pharmacological profile similar with camptothecin. (C) 2011 Elsevier Ltd. All rights reserved. |
| WOS关键词 | DNA-TOPOISOMERASE-I ; CAMPTOTHECIN ANALOGS ; INHIBITION ; RING ; VITRO |
| 资助项目 | Major Project of Chinese National Programs for Fundamental Research and Development[2009CB918404] ; National Science & Technology Major Project "Key New Drug Creation and Manufacturing Program''[2009ZX09301-001] ; National Science & Technology Major Project "Key New Drug Creation and Manufacturing Program''[2009ZX09103-065] ; Natural Science Foundation of China[30725046] ; Natural Science Foundation of China[81021062] ; Natural Science Foundation of China[90813034] ; Program of Shanghai Subject Chief Scientist[10XD1405100] |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000288245100035 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/278575]  |
| 专题 | 药理学第一研究室 中科院受体结构与功能重点实验室 新药研究国家重点实验室 药物化学研究室 |
| 通讯作者 | Geng, Meiyu |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Div Antitumor Pharmacol, Shanghai 201203, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, Dept Med Chem, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Jiao, Yu,Liu, Hongchun,Geng, Meiyu,et al. Synthesis and antitumor activity of 10-arylcamptothecin derivatives[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2011,21(7):2071-2074. |
| APA | Jiao, Yu,Liu, Hongchun,Geng, Meiyu,&Duan, Wenhu.(2011).Synthesis and antitumor activity of 10-arylcamptothecin derivatives.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,21(7),2071-2074. |
| MLA | Jiao, Yu,et al."Synthesis and antitumor activity of 10-arylcamptothecin derivatives".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 21.7(2011):2071-2074. |
入库方式： OAI收割
来源：上海药物研究所
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