Potent inhibition of checkpoint kinase activity by a hymenialdisine-derived indoloazepine

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• 作者：Sharma ; Vasudha ; Tepe ; Jetze J.
• 关键词：Hymenialdisine ; Kinase ; Checkpoint ; Chk2 ; Apoptosis
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2004
• 出版时间：August 16, 2004
• 年：2004
• 卷：14
• 期：16
• 页码：4319-4321
• 全文大小：245 K

文摘

The marine sponge metabolite hymenialdisine is a potent inhibitor of a variety of kinases including MEK-1, GSK-3β, and CK1. In addition, hymenialdisine and debromohymenialdisine exhibit inhibition of the G₂ cell cycle checkpoint at micromolar concentrations. We report herein the potent inhibition of cell cycle kinase Chk2 by the indolic-hymenialdisine indoloazepine 1 (IC₅₀