Design, synthesis and biological evaluation of novel homocamptothecin analogues as potent antitumor agents
文献类型：期刊论文
| 作者 | Wang, Lei1; Xie, Shao2; Ma, Longjun1; Chen, Yi2 ; Lu, Wei1
|
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY
 |
| 出版日期 | 2015-05-01 |
| 卷号 | 23期号:9页码:1950-1962 |
| 关键词 | Homocamptothecin Lactone stability Water solubility Anticancer drug |
| ISSN号 | 0968-0896 |
| DOI | 10.1016/j.bmc.2015.03.031 |
| 文献子类 | Article |
| 英文摘要 | Fifteen novel homocamptothecin derivatives with alpha-OMe substituted E-rings were designed and synthesized. All of the derivatives exhibited similar or superior cytotoxicities compared with that of SN-38, and they inhibited Topo I activity in a cell-free assay in a manner similar to that of SN-38, confirming that they represent a new class of Topo I inhibitors. Notably, the water soluble compound 36o (1.2 mg/mL) exhibited increased lactone stability, and at 0.5 mg/kg and 3.0 mg/kg, it demonstrated significant antitumor activity in mice bearing a xenograft model using human colon cancer cell line HT-29. On the basis of these positive results, further development of 36o-related compounds as potential anticancer clinical trial candidates is definitely warranted. (C) 2015 Elsevier Ltd. All rights reserved. |
| WOS关键词 | RING-MODIFIED CAMPTOTHECIN ; TOPOISOMERASE-I ; LACTONE RING ; CHEMICAL-MODIFICATION ; INHIBITORY-ACTIVITIES ; LUOTONIN-A ; DERIVATIVES ; 7-ETHYLCAMPTOTHECIN ; 20(S)-CAMPTOTHECIN ; NSC-100880 |
| 资助项目 | National Natural Science Foundation of China[81172936] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000352698700005 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/276558]  |
| 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 |
| 通讯作者 | Chen, Yi |
| 作者单位 | 1.E China Normal Univ, Sch Chem & Mol Engn, Shanghai 200062, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Div Antitumor Pharmacol, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Wang, Lei,Xie, Shao,Ma, Longjun,et al. Design, synthesis and biological evaluation of novel homocamptothecin analogues as potent antitumor agents[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2015,23(9):1950-1962. |
| APA | Wang, Lei,Xie, Shao,Ma, Longjun,Chen, Yi,&Lu, Wei.(2015).Design, synthesis and biological evaluation of novel homocamptothecin analogues as potent antitumor agents.BIOORGANIC & MEDICINAL CHEMISTRY,23(9),1950-1962. |
| MLA | Wang, Lei,et al."Design, synthesis and biological evaluation of novel homocamptothecin analogues as potent antitumor agents".BIOORGANIC & MEDICINAL CHEMISTRY 23.9(2015):1950-1962. |
入库方式： OAI收割
来源：上海药物研究所
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