Peumusolide A, unprecedented NES non-antagonistic inhibitor for nuclear export of MEK

Satoru Tamura; Yuuhi Hattori; Masafumi Kaneko; Nobuhiro Shimizu; Susumu Tanimura; Michiaki Kohno; Nobutoshi Murakami

doi:10.1016/j.tetlet.2010.01.068

Peumusolide A, unprecedented NES non-antagonistic inhibitor for nuclear export of MEK

Satoru Tamura, Yuuhi Hattori, Masafumi Kaneko, Nobuhiro Shimizu, Susumu Tanimura, Michiaki Kohno, Nobutoshi Murakami

SCI - Chemistry

Research output: Contribution to journal › Article › peer-review

8 Citations (Scopus)

Abstract

A new polyketide peumusolide A was disclosed as an unprecedented NES non-antagonistic inhibitor for nuclear export of MEK, a promising scaffold for antitumor agents with novel mechanism of action, from Peumus boldus Molina. The absolute stereostructure as well as optical purity was established by use of the two synthesized enantiomeric model lactones. In addition, the Δε values in their CD spectra were demonstrated to be the conclusive index for determination of not only configuration at C-3 but also optical purity of natural congeneric polyketides. Peumusolide A was revealed to show NES non-antagonistic action by the biotinylated probe and to inhibit proliferation of MEK-activated tumor cells selectively.

Original language	English
Pages (from-to)	1678-1681
Number of pages	4
Journal	Tetrahedron Letters
Volume	51
Issue number	13
DOIs	https://doi.org/10.1016/j.tetlet.2010.01.068
Publication status	Published - 2010 Mar 31

ASJC Scopus subject areas

Biochemistry
Drug Discovery
Organic Chemistry

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10.1016/j.tetlet.2010.01.068

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abstract = "A new polyketide peumusolide A was disclosed as an unprecedented NES non-antagonistic inhibitor for nuclear export of MEK, a promising scaffold for antitumor agents with novel mechanism of action, from Peumus boldus Molina. The absolute stereostructure as well as optical purity was established by use of the two synthesized enantiomeric model lactones. In addition, the Δε values in their CD spectra were demonstrated to be the conclusive index for determination of not only configuration at C-3 but also optical purity of natural congeneric polyketides. Peumusolide A was revealed to show NES non-antagonistic action by the biotinylated probe and to inhibit proliferation of MEK-activated tumor cells selectively.",

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T1 - Peumusolide A, unprecedented NES non-antagonistic inhibitor for nuclear export of MEK

AU - Tamura, Satoru

AU - Hattori, Yuuhi

AU - Kaneko, Masafumi

AU - Shimizu, Nobuhiro

AU - Tanimura, Susumu

AU - Kohno, Michiaki

AU - Murakami, Nobutoshi

PY - 2010/3/31

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Peumusolide A, unprecedented NES non-antagonistic inhibitor for nuclear export of MEK

Abstract

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