Microwave expedited synthesis of 5-aminocamptothecin analogs: Inhibitors of hypoxia inducible factor HIF-1α

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• 作者：Joelle Torregrossa ; Glenn J. Bubley ; Graham B. Jones
• 关键词：Camptothecin ; Anticancer ; Hypoxia ; HIF ; Microwave
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2006
• 出版时间：1 December 2006
• 年：2006
• 卷：16
• 期：23
• 页码：6082-6085
• 全文大小：163 K

文摘

A series of 5-aminosubstituted camptothecin analogs were prepared from the corresponding 5-hydroxycamptothecin using microwave irradiation. The analogs were assayed for ability to inhibit the action of hypoxia inducible factors (HIF-1α and HIF-2α). The 5-fluoroethyl analog showed potent inhibitory activity and is now the focus of ongoing pathway analysis and potential as an antiproliferative agent.