title: Arteminolides B, C, and D, new inhibitors of farnesyl protein transferase from Artemisia argyi.
abstract: Arteminolides B-D (2-4), new farnesyl protein transferase inhibitors, were isolated together with a known arteminolide A (1) and new regioisomers (5-7) of the compounds from the aerial parts of Artemisia argyi. Structures of these compounds were elucidated by spectroscopic methods and chemical conversion. Arteminolides inhibited the farnesyl protein transferase with IC(50) values of 0.7-1 microM, while the regioisomers 5-7 were inactive. In addition, it was proved that the exocyclic double bond of sesquiterpene lactone did not affect the inhibitory activity of arteminolide. The effects of compound 2 on H-Ras processing and cellular growth in H-ras-transformed cells were also evaluated.
authors.affiliation: Marine Natural Products Laboratory, Korea Ocean Research & Development Institute, P.O. Box 29 Ansan, Seoul 425-600, Republic of Korea.
authors.forename: Seung-Ho
authors.initials: SH
authors.lastname: Lee
authors.forename: Hyae-Kyeong
authors.initials: HK
authors.lastname: Kim
authors.forename: Jeong-Min
authors.initials: JM
authors.lastname: Seo
authors.forename: Hyun-Mi
authors.initials: HM
authors.lastname: Kang
authors.forename: Jong Han
authors.initials: JH
authors.lastname: Kim
authors.forename: Kwang-Hee
authors.initials: KH
authors.lastname: Son
authors.forename: Heesoon
authors.initials: H
authors.lastname: Lee
authors.forename: Byoung-Mog
authors.initials: BM
authors.lastname: Kwon
authors.forename: Jongheon
authors.initials: J
authors.lastname: Shin
authors.forename: Youngwan
authors.initials: Y
authors.lastname: Seo
mesh_terms: D000818:Animals; D019306:Artemisia / Q000737:chemistry*; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D011905:Genes, ras / Q000235:genetics; D007783:Lactones / Q000737:chemistry / Q000302:isolation & purification*; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D008968:Molecular Conformation; D015394:Molecular Structure; D041681:NIH 3T3 Cells; D010084:Oxidation-Reduction; D017368:Protein Prenylation; D012717:Sesquiterpenes / Q000737:chemistry / Q000302:isolation & purification*; D014166:Transferases / Q000037:antagonists & inhibitors* / Q000378:metabolism*
chemical_list: D004791:Enzyme Inhibitors; D007783:Lactones; D012717:Sesquiterpenes; C484914:arteminolide A; C484912:arteminolide B; C484913:arteminolide C; D014166:Transferases