Design, synthesis and anti-malarial activities of synthetic analogs of biselyngbyolide B, a Ca2+ pump inhibitor from marine cyanobacteria. Issue 3 (1st February 2018)

• Record Type: Journal Article
• Authors: Sato, Eisuke; Morita, Maho; Ogawa, Haruo; Iwatsuki, Masato; Hokari, Rei; Ishiyama, Aki; Ōmura, Satoshi; Iwasaki, Arihiro; Suenaga, Kiyotake
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 28:Issue 3(2018)
• Page Start: 298
• Page End: 301
• Publication Date: 2018-02-01
• Subjects: Biselyngbyaside -- Biselyngbyolide -- SERCA -- PfATP6 -- Structure–activity relationships; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2017.12.050
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: 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.