Synthesis of novel benzo-fused heteroaryl derivatives as Ca 2+/calmodulin-dependent protein kinase II inhibitors

Masafumi Komiya, Shigehiro Asano, Nobuyuki Koike, Erina Koga, Junetsu Igarashi, Shogo Nakatani, Yoshiaki Isobe

    Research output: Contribution to journalArticlepeer-review

    6 Citations (Scopus)


    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.

    Original languageEnglish
    Pages (from-to)1094-1097
    Number of pages4
    JournalChemical and Pharmaceutical Bulletin
    Issue number10
    Publication statusPublished - Oct 2013

    All Science Journal Classification (ASJC) codes

    • Chemistry(all)
    • Drug Discovery

    Fingerprint Dive into the research topics of 'Synthesis of novel benzo-fused heteroaryl derivatives as Ca <sup>2+</sup>/calmodulin-dependent protein kinase II inhibitors'. Together they form a unique fingerprint.

    Cite this