0000000000262540

AUTHOR

K. Tan

showing 2 related works from this author

New ursolic and betulinic derivatives as potential cytotoxic agents.

2003

Fifteen new ursolic and betulinic triterpenoids, bearing various functionalities at C-3 and C-28 were synthesized as potential cytotoxic agents. All compounds were obtained by a hemisynthetic route via ursolic and betulinic acids. Preliminary screening of these compounds on human HT 29 colon cancer cells revealed inhibitory activity for three of them. Beta-D-Glucopyranosyl-3beta-hydroxyurs-12(13)-en-28-oate 1c, 3beta-3-(3-pyridyl)-prop-2-enoyloxyurs-12(13)-en-28-oic acid 1i and the potassium salt of 3beta-cinnamoyloxylup-20(29)-en-28-oic acid 2d demonstrated cytotoxic activity in the micromolar range: 8.0, 45.0 and 8.0 microM, respectively.

PharmacologyMolecular StructureStereochemistryCell SurvivalAntineoplastic AgentsGeneral MedicineTriterpeneschemistry.chemical_compoundInhibitory Concentration 50Structure-Activity RelationshipTriterpenoidUrsolic acidchemistryBetulinic acidDrug DiscoveryCytotoxic T cellHumansDrug Screening Assays AntitumorBetulinic AcidCytotoxicityPentacyclic TriterpenesHT29 CellsJournal of enzyme inhibition and medicinal chemistry
researchProduct

A review of natural and modified betulinic, ursolic and echinocystic acid derivatives as potential antitumor and anti-HIV agents.

2003

The aim of this review is to update current knowledge on the betulinic, ursolic and echinocystic acids and their natural and semisynthetic analogs, focussing on their cytotoxic and anti-HIV activities. Then, the last results of the authors' team on unusual semisynthetic derivatives of these triterpenoids will be presented in order to establish structure/activity relationships.

PharmacologyMolecular StructureAnti hivChemistryAnti-HIV AgentsTumor cellsAntineoplastic AgentsGeneral MedicinePharmacologyTriterpenesStructure-Activity RelationshipTriterpenoidDrug DiscoveryHIV-1Tumor Cells CulturedStructure–activity relationshipHumansEchinocystic acidOleanolic AcidBetulinic AcidPentacyclic TriterpenesHT29 CellsMini reviews in medicinal chemistry
researchProduct