0000000000140428

AUTHOR

Kuo Hsiung Lee

showing 8 related works from this author

Anti-HIV Agents Derived from the ent-Kaurane Diterpenoid Linearol

2002

Twenty-six semisynthetic ent-kaurane derivatives of linearol (1) have been investigated for their anti-HIV effects. Five compounds (4, 7, 11, 25, and 26) showed significant activity against HIV replication in H9 lymphocyte cells with EC(50) values in the range <0.1-3.11 microg/mL. With TI values of 163 and 184, compounds 4 and 25 are especially promising for further development as potential anti-HIV agents.

Magnetic Resonance SpectroscopyAnti-HIV AgentsStereochemistryLymphocyteEnt kaurane diterpenoidHuman immunodeficiency virus (HIV)Pharmaceutical ScienceBiologymedicine.disease_causeAnalytical Chemistrychemistry.chemical_compoundDrug DiscoverymedicineCombinatorial Chemistry TechniquesHumansLymphocytesPharmacologyMolecular StructureAnti hivOrganic ChemistryHIVbiology.organism_classificationIn vitroTerpenoidmedicine.anatomical_structureComplementary and alternative medicinechemistryLentivirusSideritisMolecular MedicineDiterpenesDiterpeneJournal of Natural Products
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Cytotoxic activity of some natural and syntetic sesquiterpene lactones

2006

Several natural and synthetic sesquiterpene lactones with different skeletons were tested and found to be active against nine cancer cell lines. Elemane (4), heliangolane (5) and their hydroxy analogues 9 and 10, all containing an α,β-unsaturated aldehyde substituent, were the most potent compounds.

StereochemistrySubstituentPharmaceutical ScienceCentaureaPharmacognosySesquiterpeneAldehydeANTITUMOR AGENTSAnalytical Chemistrychemistry.chemical_compoundInhibitory Concentration 50LactonesStructure-Activity RelationshipCell Line TumorDrug DiscoveryStructure–activity relationshipOrganic chemistryCytotoxic T cellHumansCENTAUREA-PAUICytotoxicityPharmacologychemistry.chemical_classificationBiological ProductsMolecular StructureDERIVATIVESOrganic ChemistryCNICINSettore CHIM/06 - Chimica OrganicaAntineoplastic Agents PhytogenicComplementary and alternative medicinechemistryMolecular MedicineSesquiterpenesLactone
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Cytotoxic geranylflavonoids from Bonannia graeca

2011

The analysis of the aerial parts of Bonannia graeca led to the isolation and characterization of two new polar geranylated flavonoids (6 and 7). The structure elucidation was performed by extensive spectroscopic methods (1D and 2D NMR) and comparison with literature data. All natural flavonoids isolated from B. graeca (1–7) and some synthetic derivatives (8–11) were tested for cytotoxic activity against four human tumor cell lines. Preliminary structure-activity relationship correlations are discussed.

Synthetic derivativesStereochemistryChemical structurePlant ScienceHorticultureBiochemistryArticleStructure-Activity RelationshipBonannia graecaCell Line TumorHumansCytotoxic T cellStructure–activity relationshipSettore BIO/15 - Biologia FarmaceuticaGeranylflavonoidsMolecular BiologyFlavonoidsApiaceaeMolecular StructurebiologyCytotoxic activityfungiEuphorbiaceaefood and beveragesGeneral MedicineSettore CHIM/06 - Chimica OrganicaPlant Components Aerialbiology.organism_classificationAntineoplastic Agents PhytogenicHuman tumorTwo-dimensional nuclear magnetic resonance spectroscopyApiaceae
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Cytotoxic Activity of Some Natural and Synthetic ent-Kauranes

2007

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.

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 KauraneJournal of Natural Products
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The Cytotoxic Properties of Natural Coumarins Isolated from Roots ofFerulago campestris(Apiaceae) and of Synthetic Ester Derivatives of Aegelinol

2009

Grandivittin (1), agasyllin (2), aegelinol benzoate (3) and felamidin (20), four natural coumarins isolated from Ferulago campestris, and several synthetic ester derivatives of aegelinol (4) were tested against four tumor cell lines. Some of them were shown to be marginally cytotoxic against the A549 lung cancer cell line.

PharmacologyEster derivativesfood.ingredientApiaceaeStereochemistryPlant compositionPlant ScienceGeneral MedicineBiologybiology.organism_classificationFerulago campestrisFerulagofoodComplementary and alternative medicineDrug DiscoveryCytotoxic T cellOrganic chemistryNatural Product Communications
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New oxidative derivatives of atractyligenin and their cytotoxic activity

2006

ent-Kauranes are naturally occurring diterpenoids isolated from several families, such as Asteraceae and Lamiaceae. These compounds have attracted interest because of their structures and their biological activities as anti-tumorals, anti-HIV and anti-bacterials [1]. Extensive chemical work [2] was carried out on the structure of atractyligenin, the nor-diterpene aglycone of the glucoside atractyloside, occurring, together with its diterpene homologous carboxy-atractyloside, in the root of Atractylis gummifera L. (Compositae). The interest for these compounds was stimulated by the high toxicity [3] of both glucosides, responsible of many deadly poisoning in past time. Due to the 15-hydroxyl…

PharmacologyChemistryOrganic ChemistryPharmaceutical ScienceOxidative phosphorylationSettore CHIM/06 - Chimica OrganicaAtractyligeninAnalytical ChemistryComplementary and alternative medicineChemical engineeringBiochemistryoxidative atractyligenin cytotoxic activityDrug DiscoveryMolecular MedicineCytotoxic T cell
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Cytotoxic activity of some natural and synthetic guaianolides

2005

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.

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
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Acid Rearrangment of Epoxy-germacranolides and Absolute Configuration of 1β,10α-Epoxy-salonitenolide

2010

The acid-catalyzed cyclization of mono epoxides of cnicin acetonide (3) was investigated. Several 6,12-eudesmanolides were obtained, and their stereochemistry established by extensive spectroscopic analyses. Chemical correlations also led to the assignment of the absolute configuration of 1β,10α-epoxy-salonitenolide (13), a previously isolated natural product. The cytotoxic activities of some compounds were determined against A549 and MCF-7 tumor cell lines. The esterified germacranolides 2–6 were selectively cytotoxic against the MCF-7 breast cancer cell line.

PharmacologyNatural productStereochemistryAbsolute configurationSalonitenolidePlant ScienceGeneral MedicineEpoxyAcetonideCnicinchemistry.chemical_compoundComplementary and alternative medicineBreast cancer cell linechemistryvisual_artDrug Discoveryvisual_art.visual_art_mediumOrganic chemistryCytotoxicityNatural Product Communications
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