Structure and activity relationship of 2-(substituted benzoyl)- hydroxyindoles as novel CaMKII inhibitors

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

Research output: Contribution to journalArticle

4 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)1456-1458
Number of pages3
JournalBioorganic and Medicinal Chemistry Letters
Volume21
Issue number5
DOIs
Publication statusPublished - Mar 1 2011
Externally publishedYes

Fingerprint

Calcium-Calmodulin-Dependent Protein Kinase Type 2
Structure-Activity Relationship
Screening
Throughput

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

Cite this

Structure and activity relationship of 2-(substituted benzoyl)- hydroxyindoles as novel CaMKII inhibitors. / Komiya, Masafumi; Asano, Shigehiro; Koike, Nobuyuki; Koga, Erina; Igarashi, Junetsu; Nakatani, Shogo; Isobe, Yoshiaki.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 21, No. 5, 01.03.2011, p. 1456-1458.

Research output: Contribution to journalArticle

Komiya, Masafumi ; Asano, Shigehiro ; Koike, Nobuyuki ; Koga, Erina ; Igarashi, Junetsu ; Nakatani, Shogo ; Isobe, Yoshiaki. / Structure and activity relationship of 2-(substituted benzoyl)- hydroxyindoles as novel CaMKII inhibitors. In: Bioorganic and Medicinal Chemistry Letters. 2011 ; Vol. 21, No. 5. pp. 1456-1458.
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AU - Isobe, Yoshiaki

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