6533b7d0fe1ef96bd125ba6f
RESEARCH PRODUCT
Synthesis and structure-activity relationship studies of cytotoxic cinnamic alcohol derivatives.
Yongping YuLeixiang YangHongbin ZouYu ZhaoLiang ZhangLiuqing YangJoachim Stöckigtsubject
StereochemistryCell SurvivalPropanolsAlcoholAntineoplastic AgentsHL-60 CellsPlant ScienceConjugated systemBiochemistryAnalytical ChemistryHeLachemistry.chemical_compoundStructure-Activity RelationshipCell Line TumorStructure–activity relationshipCytotoxic T cellHumansCytotoxicityCinnamyl alcoholbiologyChemistryOrganic Chemistrybiology.organism_classificationCell cultureDrug Screening Assays AntitumorHeLa Cellsdescription
Three series of di- and trisubstituted derivatives of cinnamic alcohol and its conjugated dienol analogues were designed and synthesised. The derivatives were screened for cytotoxicity against nine tumour cell lines: KB, A549, Hela, CNE, PC-3, BEL-7404, HL-60, BGC823 and P388D1. Most of the cinnamic alcohol derivatives showed cytotoxic activity. The compound 7-(4',5'-dichlorobenzyloxy)-6,8-dihydroxycinnamic alcohol (55) exhibited significant cytotoxicity to seven human tumour cell lines on a micromolar range, especially with regard to the KB and P388D1 cell lines, showing IC(50) values of 0.4 and 0.5 µM, respectively. The structure-activity relationships of the derivatives are discussed.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2011-02-01 | Natural product research |