Sesquiterpene lactones, inhibitors of farnesyl protein transferase, isolated from the flower of Artemisia sylvatica

Citation
Sh. Lee et al., Sesquiterpene lactones, inhibitors of farnesyl protein transferase, isolated from the flower of Artemisia sylvatica, TETRAHEDRON, 56(27), 2000, pp. 4711-4715
Citations number
15
Categorie Soggetti
Chemistry & Analysis","Organic Chemistry/Polymer Science
Journal title
TETRAHEDRON
ISSN journal
00404020 → ACNP
Volume
56
Issue
27
Year of publication
2000
Pages
4711 - 4715
Database
ISI
SICI code
0040-4020(20000630)56:27<4711:SLIOFP>2.0.ZU;2-D
Abstract
Five sesquiterpene lactones, 8-acetylarteminolide (1), artanomaloide (2), a rteminones (3 and 4), and dehydromatricarin (5), were isolated from the met hanolic extract of the flower of Artemisia sylvatica and characterized on t he basis of their spectral data. New sesquiterpene lactone 1 was identified as a configurational isomer of artanomaloide (2), and the new arteminones 3 and 4 are determined as stereoisomers. 8-Acetylarteminolide (1) strongly inhibited FPTase with an IC50 of 1.8 mu M, however, the other sesquiterpene lactones mildly inhibited the transferase with an IC50 of 22-300 mu M. (C) 2000 Elsevier Science Ltd. All rights reserved.