The Journal of Organic Chemistry · 2002 · 68 citations · 1 references
PharmacyMedicinal ChemistryPharmacologyDrug DiscoveryEnzymologyStructure-activity RelationshipsEnzyme DiscoveryEnzyme InhibitionEnzyme TargetsMedicinal PlantsNatural Product Drug DiscoveryStructure-activity Relationship AnalysisCellular GrowthEnzyme Inhibition ScreeningTransferase Discovery
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.
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