Design, synthesis and anti-malarial activities of synthetic analogs of biselyngbyolide B, a Ca 2+ pump inhibitor from marine cyanobacteria

Eisuke Sato, Maho Morita, Haruo Ogawa, Masato Iwatsuki, Rei Hokari, Aki Ishiyama, Satoshi Ōmura, Arihiro Iwasaki, Kiyotake Suenaga

Research output: Contribution to journalArticle

4 Citations (Scopus)

Abstract

Biselyngbyaside, an 18-membered macrolide glycoside from marine cyanobacteria, and its derivatives are known to be sarco/endoplasmic reticulum Ca 2+ ATPase (SERCA) inhibitors. Recently, a SERCA orthologue of the malaria parasite, PfATP6, has attracted attention as a malarial drug target. To provide a novel drug lead, we designed new synthetic analogs of biselyngbyolide B, the aglycone of biselyngbyaside, based on the co-crystal structure of SERCA with biselyngbyolide B, and synthesized them using the established synthetic route for biselyngbyolide B. Their biological activities against malarial parasites were evaluated.

Original languageEnglish
Pages (from-to)298-301
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume28
Issue number3
DOIs
Publication statusPublished - Feb 1 2018
Externally publishedYes

Keywords

  • Biselyngbyaside
  • Biselyngbyolide
  • PfATP6
  • SERCA
  • Structure–activity relationships

ASJC Scopus subject areas

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

Fingerprint Dive into the research topics of 'Design, synthesis and anti-malarial activities of synthetic analogs of biselyngbyolide B, a Ca <sup>2+</sup> pump inhibitor from marine cyanobacteria'. Together they form a unique fingerprint.

Cite this