6533b860fe1ef96bd12c3137
RESEARCH PRODUCT
Synthesis and cytotoxic activity of novel C7-functionalized spongiane diterpenes.
Jelver SierraManuel ArnóRamón J. ZaragozáMiguel A. GonzálezLiliana Betancur-galvissubject
StereochemistryClinical BiochemistryPharmaceutical ScienceAntineoplastic AgentsButyrateBiochemistryChemical synthesisHeLachemistry.chemical_compoundInhibitory Concentration 50Structure-Activity RelationshipCell Line TumorDrug DiscoveryStructure–activity relationshipHumansCytotoxicityMolecular Biologychemistry.chemical_classificationbiologyMolecular StructureOrganic Chemistrybiology.organism_classificationButyrateschemistryMolecular MedicineHemiacetalDiterpeneDiterpenesDrug Screening Assays AntitumorLactoneHeLa Cellsdescription
Based on two lead cytotoxic spongiane diterpenes, a new series of C7-oxygenated derivatives were synthesized and evaluated for their antitumor activity in vitro against the cancer cell lines HeLa and HEp-2. In general, introduction of either hydroxyl or acetoxy groups at C-7 did not improve the resultant cytotoxicity, while the presence of a butyrate ester led to more active compounds (CC(50)=4.0-9.5 microM).
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2003-07-01 | Bioorganicmedicinal chemistry |