Structure and activity relationship of 2-(substituted benzoyl)-hydroxyindoles as novel CaMKII inhibitors |
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Authors: | Komiya Masafumi Asano Shigehiro Koike Nobuyuki Koga Erina Igarashi Junetsu Nakatani Shogo Isobe Yoshiaki |
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Institution: | Chemistry Research Laboratories, Dainippon Sumitomo Pharma Co., Ltd, 3-1-98 Kasugade Naka, Konohana-ku, Osaka 554-0022, Japan |
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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. |
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Keywords: | CaMKII Indole Kinase Inhibitor Calmodulin |
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