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
  • 1. Chemistry Research Laboratories, Dainippon Sumitomo Pharma Co., Ltd, Konohana-ku, Osaka, Japan. [email protected]
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.