6533b857fe1ef96bd12b3b1a

RESEARCH PRODUCT

Cytotoxic activity of some natural and synthetic guaianolides

Antonella MaggioSergio RosselliMaurizio BrunoKenneth F. BastowKuo Hsiung LeeRosa Angela Raccuglia

subject

PaclitaxelStereochemistryPharmaceutical ScienceEpoxideSesquiterpeneAnalytical Chemistrychemistry.chemical_compoundStructure-Activity RelationshipDrug DiscoveryTumor Cells CulturedPotencyHumansCytotoxicityPharmacologychemistry.chemical_classificationMolecular StructureChemistryOrganic ChemistrySettore CHIM/06 - Chimica OrganicaAntineoplastic Agents PhytogenicIn vitroTerpenoidCentaurea Asteraceae sesquiterpene lactonesComplementary and alternative medicinePaclitaxelMolecular MedicineDrug Screening Assays AntitumorSesquiterpenesLactone

description

Several natural guaianolides and synthetic derivatives of repin (1) were tested and found to be active against tumor cell replication. Repin (1) and both mono- and di-halohydrin analogues (2, 7-9, 11, 12) showed significant antitumor potency. A more effective compound (17) was obtained by esterificating repin with the paclitaxel side chain.

yearjournalcountryeditionlanguage
2005-07-26
10.1021/np0500575http://hdl.handle.net/10447/9794