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Title: Structure and activity relationship of 2-(substituted benzoyl)-hydroxyindoles as novel CaMKII inhibitors. Author: Komiya M, Asano S, Koike N, Koga E, Igarashi J, Nakatani S, Isobe Y. Journal: Bioorg Med Chem Lett; 2011 Mar 01; 21(5):1456-8. PubMed ID: 21292482. Abstract: A series of novel 2-substituted-5-hydroxyindoles were synthesized and evaluated for their inhibitory activity against CaMKII. Structure and activity relationship results indicated that potent inhibitory activity could be achieved by modification at the para-position of the phenyl ring of the high throughput screening hit compound 2. Among the prepared compounds, we identified 14 as a novel CaMKII inhibitor with an activity stronger than that of KN-93, a known CaMKII inhibitor.[Abstract] [Full Text] [Related] [New Search]