Design, synthesis and anti-malarial activities of synthetic analogs of biselyngbyolide B, a Ca 2+ pump inhibitor from marine cyanobacteria
Design, synthesis and anti-malarial activities of synthetic analogs of biselyngbyolide B, a Ca 2+ pump inhibitor from marine cyanobacteria
复制标题
Biselngbyolide B 的合成类似物（一种来自海洋蓝藻的 Ca 2 泵抑制剂）的设计、合成和抗疟活性
DOI：
10.1016/j.bmcl.2017.12.050
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发表时间：
2018
影响因子：
2.7
通讯作者：
Suenaga Kiyotake
中科院分区：
文献类型：
--
作者：
Sato Eisuke;Morita Maho;Ogawa Haruo;Iwatsuki Masato;Hokari Rei;Ishiyama Aki;?mura Satoshi;Iwasaki Arihiro;Suenaga Kiyotake
Biselyngbyaside是一种来自海洋蓝藻菌的18元大环内酯糖苷，其衍生物被认为是sarco/内质网Ca2+ atp酶（SERCA）抑制剂。最近，疟原虫的SERCA同源物PfATP6作为一种疟疾药物靶点引起了人们的关注。为了提供一种新的药物先导，我们基于SERCA与二飞蓟苷内酯B的共晶结构，设计了新的二飞蓟苷内酯B的合成类似物，并利用已建立的二飞蓟苷内酯B的合成路线进行了合成，并评价了它们对疟原虫的生物活性。
Biselyngbyaside, an 18-membered macrolide glycoside from marine cyanobacteria, and its derivatives are known to be sarco/endoplasmic reticulum Ca2+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.