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 C-18/19 diastereomers, simplified analogs without the peptide unit, and aglycones. Evaluations...

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Bibliographic Details
Published in:Bulletin of the Chemical Society of Japan 2024-07, Vol.97 (7)
Main Authors: Kurisawa, Naoaki, Teranuma, Kazuya, Noto, Akari, Iwasaki, Arihiro, Kabashima, Yoshiki, Nakajima, Rie, Toyoshima, Chikashi, Suenaga, Kiyotake
Format: Article
Language:English
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Summary: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 C-18/19 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 C-18/19, peptide, and the sugar unit contribute to each bioactivity.
ISSN:0009-2673
1348-0634
DOI:10.1093/bulcsj/uoae070