Poly (ethylene glycol) prodrug for anthracyclines via N-Mannich base linker: Design, synthesis and biological evaluation
文献类型：期刊论文
| 作者 | Zhao, Yong-Jiang1,2; Wei, Wei1,2; Su, Zhi-Guo1; Ma, Guang-Hui1 |
| 刊名 | INTERNATIONAL JOURNAL OF PHARMACEUTICS
 |
| 出版日期 | 2009-09-08 |
| 卷号 | 379期号:1页码:90-99 |
| 关键词 | PEGylated prodrug Anthracycline anticancer drug N-Mannich base |
| ISSN号 | 0378-5173 |
| 通讯作者 | Ma, GH |
| 英文摘要 | Poly(ethylene glycol)s (PEGs) are potential drug carriers for improving the therapeutic index of anticancer agents. In this work, a novel methodology for constructing PEG prodrug of anthracycline anticancer drugs was developed based on N-Mannich base of salicylamide and its 2-acyloxymethylated derivative. The resultant conjugates first subjected to in vitro hydrolysis testing, which revealed the release behavior of newly synthesized PEG prodrugs could be adjusted by the status of 2-hydroxy group of salicylamide. These PEG prodrugs also demonstrated superior cytotoxicity in antiproliferative assay. O-blocked doxorubicin prodrug with PEG20k as carrier was selected for further in vivo assessments and presented longer circulating life in pharmacokinetic experiment. This high molecular prodrug was also found to be more efficacious against S-180 xenografted tumor than equivalent amount of doxorubicin. (C) 2009 Elsevier B.V. All rights reserved. |
| WOS标题词 | Science & Technology ; Life Sciences & Biomedicine |
| 类目[WOS] | Pharmacology & Pharmacy |
| 研究领域[WOS] | Pharmacology & Pharmacy |
| 关键词[WOS] | DRUG-DELIVERY SYSTEMS ; IN-VITRO CYTOTOXICITY ; POLYMERIC PRODRUGS ; ANTITUMOR-ACTIVITY ; DOXORUBICIN ; THERAPEUTICS ; RELEASE ; COPOLYMERS ; CONJUGATE ; LINKAGES |
| 收录类别 | SCI |
| 语种 | 英语 |
| WOS记录号 | WOS:000269809600012 |
| 公开日期 | 2013-11-29 |
| 版本 | 出版稿 |
| 源URL | [http://ir.ipe.ac.cn/handle/122111/6584]  |
| 专题 | 过程工程研究所_生化工程国家重点实验室 |
| 作者单位 | 1.Chinese Acad Sci, Natl Key Lab Biochem Engn, Inst Proc Engn, Beijing 100190, Peoples R China 2.Chinese Acad Sci, Grad Univ Chinese, Beijing 100049, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zhao, Yong-Jiang,Wei, Wei,Su, Zhi-Guo,et al. Poly (ethylene glycol) prodrug for anthracyclines via N-Mannich base linker: Design, synthesis and biological evaluation[J]. INTERNATIONAL JOURNAL OF PHARMACEUTICS,2009,379(1):90-99. |
| APA | Zhao, Yong-Jiang,Wei, Wei,Su, Zhi-Guo,&Ma, Guang-Hui.(2009).Poly (ethylene glycol) prodrug for anthracyclines via N-Mannich base linker: Design, synthesis and biological evaluation.INTERNATIONAL JOURNAL OF PHARMACEUTICS,379(1),90-99. |
| MLA | Zhao, Yong-Jiang,et al."Poly (ethylene glycol) prodrug for anthracyclines via N-Mannich base linker: Design, synthesis and biological evaluation".INTERNATIONAL JOURNAL OF PHARMACEUTICS 379.1(2009):90-99. |
入库方式： OAI收割
来源：过程工程研究所
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