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

Research output: Contribution to journalArticle

7 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 languageEnglish
Pages (from-to)1678-1681
Number of pages4
JournalTetrahedron Letters
Volume51
Issue number13
DOIs
Publication statusPublished - 2010 Mar 31

ASJC Scopus subject areas

  • Biochemistry
  • Drug Discovery
  • Organic Chemistry

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    Tamura, S., Hattori, Y., Kaneko, M., Shimizu, N., Tanimura, S., Kohno, M., & Murakami, N. (2010). Peumusolide A, unprecedented NES non-antagonistic inhibitor for nuclear export of MEK. Tetrahedron Letters, 51(13), 1678-1681. https://doi.org/10.1016/j.tetlet.2010.01.068