Absoluteconfigurationofpodophyllotoxoneanditsinhibitoryactivityagainsthumanprostatecancercells
摘要: Podophyllotoxone(1)wasisolatedfromtherootsofDysosmaversipellis.Thestructurewasdeterminedbyspectroscopicanalysisincombinationwithsingle-crystalX-rayanalysis.Theabsoluteconfigurationofcompound1wasassignedbasedontheFlackparameter.ItshowedsignificantinhibitoryactivitiesagainsthumanprostatecancercellsPC3andDU145withIC50valuesbeing14.7and20.6μmol·L-1,respectively.ItalsoarrestedthecellsatG2/Mphase.Tubulinpolymerizationassayshowedthatitinhibitedthetubulinpolymerizationinadose-dependentmanner,andmoleculardockinganalysisrevealedadifferentbindingmodewithtubulinascomparedwiththoseknowntubulininhibitors. ...
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