Synthesis of novel benzo-fused heteroaryl derivatives as Ca²⁺/calmodulin-dependent protein kinase II inhibitors

Autor:	Masafumi, Komiya, Shigehiro, Asano, Nobuyuki, Koike, Erina, Koga, Junetsu, Igarashi, Shogo, Nakatani, Yoshiaki, Isobe
Rok vydání:	2013
Předmět:	Structure-Activity Relationship Indoles Benzothiazoles Calcium-Calmodulin-Dependent Protein Kinase Type 2 Protein Kinase Inhibitors Benzofurans Protein Binding
Zdroj:	Chemicalpharmaceutical bulletin. 61(10)
ISSN:	1347-5223
Popis:	Based on the structure activity relationship of 2-(4-phenoxybenzoyl)-5-hydroxyindole (1), a novel structural class of Ca²⁺/calmodulin-dependent protein kinase II (CaMKII) inhibitors were synthesized. We show in this study that the acidic proton at the N(1)-position of the indole moiety is not essential for CaMKII inhibitory activity. Among the synthesized compounds, we found the benzofuran and benzothiazole derivative as promising scaffolds for the developement of potent CaMKII inhibitors. In particular, compounds 8 and 14 inhibited CaMKII with IC₅₀ values of 24 nM and 32 nM, respectively.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=pmid________::c65a0f27dd9821e3fc88736d5501e2a9 https://pubmed.ncbi.nlm.nih.gov/24088703 Zobrazit plný text záznamu