title: Structure and activity relationship of 2-(substituted benzoyl)-hydroxyindoles as novel CaMKII inhibitors.
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.
authors.affiliation: Chemistry Research Laboratories, Dainippon Sumitomo Pharma Co., Ltd, Konohana-ku, Osaka, Japan. masafumi-komiya@ds-pharma.co.jp
authors.forename: Masafumi
authors.initials: M
authors.lastname: Komiya
authors.forename: Shigehiro
authors.initials: S
authors.lastname: Asano
authors.forename: Nobuyuki
authors.initials: N
authors.lastname: Koike
authors.forename: Erina
authors.initials: E
authors.lastname: Koga
authors.forename: Junetsu
authors.initials: J
authors.lastname: Igarashi
authors.forename: Shogo
authors.initials: S
authors.lastname: Nakatani
authors.forename: Yoshiaki
authors.initials: Y
authors.lastname: Isobe
mesh_terms: D054732:Calcium-Calmodulin-Dependent Protein Kinase Type 2 / Q000037:antagonists & inhibitors*; D004789:Enzyme Activation / Q000187:drug effects; D007211:Indoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D007211:Indoles; D047428:Protein Kinase Inhibitors; D054732:Calcium-Calmodulin-Dependent Protein Kinase Type 2