1207869-07-5Relevant articles and documents
Synthesis and structure based optimization of 2-(4-phenoxybenzoyl)-5- hydroxyindole as a novel CaMKII inhibitor
Komiya, Masafumi,Asano, Shigehiro,Koike, Nobuyuki,Koga, Erina,Igarashi, Junetsu,Nakatani, Shogo,Isobe, Yoshiaki
, p. 6840 - 6847 (2013/01/15)
Based on 2-(4-phenoxybenzoyl)-5-hydroxyindole (2), a novel structural class of CaMKII inhibitors were synthesized and further optimized. The strong acidity of the hydroxyl group and the lipophilic group at the 4 and 6-positions were found to be necessary for strong CaMKII inhibition. Compound 25 was identified as a promising compound with 50-fold more potent inhibitory activity for CaMKII than 2. Compound 25 also showed high selectivity for CaMKII over off-target kinases.