Synthesis and evaluation of biological activities of vibsanin A analogs

Wataru Matsuki, So Miyazaki, Keisuke Yoshida, Akihiro Ogura, Yukiko Sasazawa, Kenichi Takao, Siro Simizu

Research output: Contribution to journalArticle

6 Citations (Scopus)

Abstract

Vibsanin A is an 11-membered vibsane diterpenoid and is reported to induce myeloid cell differentiation via activation of protein kinase C (PKC) without tumor-promoting activity. Therefore, vibsanin A is thought to be an attractive compound for acute myeloid leukemia (AML) therapy. In this study, we synthesized vibsanin A analogs and compared the activity of these compounds for PKC activation and myeloid cell differentiation. We found that the hydroxymethyl group in vibsanin A is an important substituent to induce differentiation of AML cells. Collectively, our results showed the biochemical features of vibsanin A and provided new insights into the development of new antileukemic drugs.

Original languageEnglish
Pages (from-to)4536-4539
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume27
Issue number19
DOIs
Publication statusPublished - 2017 Oct 1

Keywords

  • Acute myeloid leukemia
  • Differentiation
  • Protein kinase C
  • Vibsanin A

ASJC Scopus subject areas

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

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