Synthesis and antitumor activity of the hexacyclic camptothecin derivatives | |
Gao, HY; Zhang, XW; Chen, Y![]() ![]() | |
刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
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2005-07-01 | |
卷号 | 15期号:13页码:3233-3236 |
关键词 | camptothecin topoisomerase I antitumor activity |
ISSN号 | 0960-894X |
DOI | 10.1016/j.bmcl.2005.04.063 |
文献子类 | Article |
英文摘要 | A series of hexacyclic camptothecin derivatives were synthesized to test for antitumor activity as topoisomerase I inhibitor. The strategy of synthesis was used for the formation of additional furan and dihydrofuran rings fused with 9- and 10-positions of camptothecin. All of the hexacyclic camptothecins were assayed for cytotoxicity against four human tumor cell lines, HL60, BEL-7402, HCT-116, and HeLa, and showed very impressive cytotoxicity activity in vitro. Enzyme activity of the hexacyclic camptothecins was evaluated, being equal or superior to that of SN-38. The stability of four compounds was assessed in human plasma. Two of these compounds were chosen to test for antitumor activity in vivo against Sarcoma-180. The results suggested that additional furan and dihydrofuran rings could improve the antitumor activity in vitro and vivo, though the stability of the lactone ring did not increase. (c) 2005 Elsevier Ltd. All rights reserved. |
WOS关键词 | DNA-TOPOISOMERASE-I ; ANALOGS ; RING |
WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
语种 | 英语 |
出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
WOS记录号 | WOS:000230062300012 |
内容类型 | 期刊论文 |
源URL | [http://119.78.100.183/handle/2S10ELR8/273840] ![]() |
专题 | 药理学第一研究室 药物化学研究室 |
通讯作者 | Lu, W |
作者单位 | Chinese Acad Sci, Shanghai Inst Mat Med, SIBS, Grad Sch, Shanghai 201203, Peoples R China |
推荐引用方式 GB/T 7714 | Gao, HY,Zhang, XW,Chen, Y,et al. Synthesis and antitumor activity of the hexacyclic camptothecin derivatives[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2005,15(13):3233-3236. |
APA | Gao, HY.,Zhang, XW.,Chen, Y.,Shen, HW.,Pang, T.,...&Lu, W.(2005).Synthesis and antitumor activity of the hexacyclic camptothecin derivatives.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,15(13),3233-3236. |
MLA | Gao, HY,et al."Synthesis and antitumor activity of the hexacyclic camptothecin derivatives".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 15.13(2005):3233-3236. |
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