Synthesis and biological evaluation of bis and monocarbonate prodrugs of 10-hydroxycamptothecins
文献类型：期刊论文
| 作者 | He, XG; Lu, W; Jiang, XQ; Cai, JC; Zhang, XW; Ding, J
|
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY
 |
| 出版日期 | 2004-08-01 |
| 卷号 | 12期号:15页码:4003-4008 |
| 关键词 | camptothecin 10-hydroxycamptothecin carbonate anti-tumor |
| ISSN号 | 0968-0896 |
| DOI | 10.1016/j.bmc.2004.06.003 |
| 文献子类 | Article |
| 英文摘要 | In an effort to improve the stability of labile lactone ring of camptothecins, the his and mono-alkyl carbonate prodrugs of 10-hydroxycamptothecins were synthesized and their chemical and enzymatical stability as well as antitumor activity were studied. The in vitro evaluation of the stability of these carbonates indicates that the 10,20-biscarbonates are firstly hydrolyzed to afford the stable 20-monocarbonates. And the 10-carbonates are not stable in human plasma, mouse plasma and pH 7.4 phosphate buffer, while the 20-carbonates are relatively stable in the three media and can be readily cleaved by porcine liver esterase. The overall toxicity of the tested carbonate against mice bearing S 180 sarcoma is much lower when compared with the parent compound, and the antitumor activity is maintained. (C) 2004 Elsevier Ltd. All rights reserved. |
| WOS关键词 | ANTITUMOR-ACTIVITY ; CAMPTOTHECIN ; DERIVATIVES ; CANCER |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000222886700006 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/274039]  |
| 专题 | 药理学第一研究室 |
| 通讯作者 | Lu, W |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, SIBS, Shanghai 201203, Peoples R China 2.Nanjing Univ, Jiangsu Prov Lab Nanotechnol, Nanjing 210093, Peoples R China |
| 推荐引用方式 GB/T 7714 | He, XG,Lu, W,Jiang, XQ,et al. Synthesis and biological evaluation of bis and monocarbonate prodrugs of 10-hydroxycamptothecins[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2004,12(15):4003-4008. |
| APA | He, XG,Lu, W,Jiang, XQ,Cai, JC,Zhang, XW,&Ding, J.(2004).Synthesis and biological evaluation of bis and monocarbonate prodrugs of 10-hydroxycamptothecins.BIOORGANIC & MEDICINAL CHEMISTRY,12(15),4003-4008. |
| MLA | He, XG,et al."Synthesis and biological evaluation of bis and monocarbonate prodrugs of 10-hydroxycamptothecins".BIOORGANIC & MEDICINAL CHEMISTRY 12.15(2004):4003-4008. |
入库方式： OAI收割
来源：上海药物研究所
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