期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 18, 期 9, 页码 2910-2915出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.03.074
关键词
topoisomerase I inhibitors; homocamptothecins; antitumor
资金
- Associazione Italiana per la Ricerca sul Cancro Funding Source: Custom
In contrast to five-membered E-ring analogues, 7-oxyiminomethyl derivatives of homocamptothecins showed ability to form stable ternary complexes with DNA and topoisomerase I. The 7-oxyiminomethyl derivatives of homocamptothecins were evaluated as a racemic mixture. Following the isolation of the two enantiomers, the 20 (R)-hydroxy isomer confirms the best activity. By using a panel of human tumor cells, all tested homocamptothecins showed a potent antiproliferative activity, correlating to the persistence of the cleavable complex. No significant difference was observed between the natural scaffold and the corresponding homocamptothecin homologue. A selected compound of this series exhibited an excellent antitumor activity against human gastrointestinal tumor xenografts. (C) 2008 Elsevier Ltd. All rights reserved.
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