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RESEARCH PRODUCT

Cytotoxic Activity of Some Natural and Synthetic ent-Kauranes

Kuo Hsiung LeeKenneth F. BastowTzu Hsuan ChenAntonella MaggioSergio RosselliGabriella BelloneMaurizio Bruno

subject

KetoneStereochemistryPharmaceutical ScienceAsteraceaeAtractylosideBiologyANTITUMOR AGENTSAnalytical Chemistrychemistry.chemical_compoundDrug DiscoveryTumor Cells CulturedHumansCytotoxic T cellCytotoxicityOvarian NeoplasmsPharmacologychemistry.chemical_classificationLamiaceaePlants MedicinalMolecular StructureDERIVATIVESOrganic ChemistryBiological activityAntineoplastic Agents PhytogenicTerpenoidIn vitroComplementary and alternative medicinechemistryBiochemistryCell cultureMolecular MedicineFemaleDrug Screening Assays AntitumorDiterpeneDiterpenes Kaurane

description

Atractyligenin (1) and several synthetic derivatives were tested and found to be active against tumor cell replication. Compound 1 was readily converted to the 2,15-diketo (3) or 15-keto (4) derivatives, which contain an alpha,beta-unsaturated ketone. Compounds 3 and 4 showed significant cytotoxic activity against all six tested cancer cell lines and were most potent against 1A9 ovarian cancer cells with EC50 values of 0.2 and 0.3 microM, respectively. These two 1-analogues are promising lead compounds for further investigation.

yearjournalcountryeditionlanguage
2007-03-24Journal of Natural Products
https://doi.org/10.1021/np060504w