2. Academic Validation
  3. Structure and activity relationship of 2-(substituted benzoyl)-hydroxyindoles as novel CaMKII inhibitors

Structure and activity relationship of 2-(substituted benzoyl)-hydroxyindoles as novel CaMKII inhibitors

  • Bioorg Med Chem Lett. 2011 Mar 1;21(5):1456-8. doi: 10.1016/j.bmcl.2011.01.012.
Masafumi Komiya 1,  Shigehiro Asano,  Nobuyuki Koike,  Erina Koga,  Junetsu Igarashi,  Shogo Nakatani,  Yoshiaki Isobe
Affiliations

Affiliation

  • 1 Chemistry Research Laboratories, Dainippon Sumitomo Pharma Co., Ltd, Konohana-ku, Osaka, Japan. masafumi-komiya@ds-pharma.co.jp
PMID: 21292482 DOI: 10.1016/j.bmcl.2011.01.012
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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