A series of camptothecin prodrugs exhibit HDAC inhibition activity
文献类型：期刊论文
| 作者 | Zhu, Qiwen2; Yu, Xumeng2; Shen, Qianqian3; Zhang, Qiumeng1,2; Su, Mingbo1; Zhou, Yubo1 ; Li, Jia1; Chen, Yi3; Lu, Wei2
|
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY
 |
| 出版日期 | 2018-09-01 |
| 卷号 | 26期号:16页码:4706-4715 |
| 关键词 | Camptothecin HDAC SAHA Prodrug |
| ISSN号 | 0968-0896 |
| DOI | 10.1016/j.bmc.2018.08.008 |
| 文献子类 | Article |
| 英文摘要 | Camptothecin plays an important role in clinical cancer treatment, and its derivatives are a favorite of pharmaceutical chemists. Herein, we have designed a series of camptothecin prodrugs that exhibit histone deacetylase (HDAC) inhibition activity based on the synergy effect between HDAC inhibitors and camptothecin derivatives. With the evaluation of stability in buffers or plasma from human or mouse model, an appropriate linker was found, so the active drug can be released efficiently and compound 21a exhibited strong anti-proliferative activity in A549 and HCT-116 cell lines. These results indicated that the well-designed prodrug can be promising in cancer treatment. |
| WOS关键词 | HISTONE DEACETYLASE INHIBITORS ; CELL LUNG-CANCER ; ANTICANCER DRUGS ; ANTITUMOR AGENTS ; TOPOISOMERASE-I ; COLON-CANCER ; 5-FLUOROURACIL ; COMBINATION ; VORINOSTAT ; EXPRESSION |
| 资助项目 | Shanghai Science and Technology Council[16DZ2280100] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000442887900012 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/279599]  |
| 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; Lu, Wei |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, Natl Ctr Drug Screening, Shanghai 201203, Peoples R China 2.East China Normal Univ, Shanghai Engn Res Ctr Mol Therapeut & New Drug De, Sch Chem & Mol Engn, 3663 North Zhongshan Rd, Shanghai 200062, Peoples R China; 3.Chinese Acad Sci, Shanghai Inst Mat Med, Div Antitumor Pharmacol, State Key Lab Drug Res, Shanghai 201203, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Zhu, Qiwen,Yu, Xumeng,Shen, Qianqian,et al. A series of camptothecin prodrugs exhibit HDAC inhibition activity[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2018,26(16):4706-4715. |
| APA | Zhu, Qiwen.,Yu, Xumeng.,Shen, Qianqian.,Zhang, Qiumeng.,Su, Mingbo.,...&Lu, Wei.(2018).A series of camptothecin prodrugs exhibit HDAC inhibition activity.BIOORGANIC & MEDICINAL CHEMISTRY,26(16),4706-4715. |
| MLA | Zhu, Qiwen,et al."A series of camptothecin prodrugs exhibit HDAC inhibition activity".BIOORGANIC & MEDICINAL CHEMISTRY 26.16(2018):4706-4715. |
入库方式： OAI收割
来源：上海药物研究所
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