强效 Ca2+ ATP 酶抑制剂 Iezoside 的结构-活性关系研究

IF 3.3 3区化学 Q2 CHEMISTRY, MULTIDISCIPLINARY

Bulletin of the Chemical Society of Japan Pub Date : 2024-07-06 DOI:10.1093/bulcsj/uoae070

Naoaki Kurisawa, Kazuya Teranuma, Akari Noto, Arihiro Iwasaki, Yoshiki Kabashima, Rie Nakajima, Chikashi Toyoshima, Kiyotake Suenaga

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引用次数: 0

摘要

Iezoside (1a) 是一种来自海洋蓝藻的新型强效肌浆/内质网 Ca2+ ATP 酶（SERCA）抑制剂。本文介绍了含有 C18/19 非对映异构体的综合艾素唑苷 (1a) 类似物、不含肽单元的简化类似物以及苷元的合成。通过评估合成的类似物对癌细胞的抗增殖活性和对 SERCA 的抑制活性，揭示了 C18/19、肽和糖单元的绝对构型对每种生物活性的影响。

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Structure-Activity Relationship Studies on Iezoside, a Highly Potent Ca2+ ATPase Inhibitor

Iezoside (1a) is a novel, potent sarco/endoplasmic reticulum Ca2+ ATPase (SERCA) inhibitor from marine cyanobacterium. This paper describes the synthesis of comprehensive iezoside (1a) analogs containing C18/19 diastereomers, simplified analogs without the peptide unit, and aglycones. Evaluations of the antiproliferative activities against cancer cells and SERCA inhibitory activities of the synthesized analogs revealed how the absolute configurations at C18/19, peptide, and the sugar unit contribute to each bioactivity.Ca2+ ATPase (SERCA) inhibitor, Structure-activity relationship, Marine natural products

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来源期刊

Bulletin of the Chemical Society of Japan 化学-化学综合

CiteScore

6.40

自引率

5.00%

发文量

194

审稿时长

3-8 weeks

期刊介绍： The Bulletin of the Chemical Society of Japan (BCSJ) is devoted to the publication of scientific research papers in the fields of Theoretical and Physical Chemistry, Analytical and Inorganic Chemistry, Organic and Biological Chemistry, and Applied and Materials Chemistry. BCSJ appears as a monthly journal online and in advance with three kinds of papers (Accounts, Articles, and Short Articles) describing original research. The purpose of BCSJ is to select and publish the most important papers with the broadest significance to the chemistry community in general. The Chemical Society of Japan hopes all visitors will notice the usefulness of our journal and the abundance of topics, and welcomes more submissions from scientists all over the world.