Bioorganic & medicinal chemistry letters

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

V Sharma, JJ Tepe

文献索引：Sharma, Vasudha; Tepe, Jetze J. Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 16 p. 4319 - 4321

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被引用次数: 58

摘要

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= 8nM).