简介:Usingfourβ-cyclodextrinderivatives,2,6-di-O-benzyl-3-O-heptanonyl-β-CD,2,6-di-O-benzyl-3-O-octanonyl-β-CD,2,3-di-O-benzyl-6-O-heptanonyl-β-CD,and2,3-di-O-benzyl-6-O-octanonyl-β-CD,aschiralstationaryphasesofcapillarygaschromatography(CGC),theenantiomersofSharplessepoxideswerewellseparated.Theenantiomerexcessvalues(e.e.%)ofsomechiralSharplessepoxideswerealsodeterminedsuccessfullyusingtheseCDs.
简介:Anovelseriesofpyrido[1,2-e]purin-4(3H)-onederivativescontainingpolarsubstituentson5'-positionweredesignedandpreparedaspotentialPDE5inhibitors.Thispaperreportsthesyntheticroutes,1H-NMRdata,andthePDE5inhibitoryactivitiesofthetargetcompounds.Thepolarpiperazinylgroupcontained(on5'-position)compound,3B2,showedthehighestactivityamongthetestedderivativesbutlesspotencythansildenafil1.
简介:Startedfrom5-hydroxy-2-pentanone,(R)(E)-3,7-dimethyl-2-octene-1,8-dioicacid,callosobruchusicacid,wassynthesizedviafivestepswithD-(-)-camphorsultamasthechiralauxiliary.Itwasofgoodopticalpurityandyield.
简介:Theeffectandmechanismofcarmustine(BCNU)combinedwithall-transretinoicacid(ATRA)ontheapoptosisofhumanglioblastomaU251cellswereinvestigatedbymeansof3-(4,5-dimethylthiazol-2-yl)-2,5-diphe-nyltetrazoliumbromide(MTT)assay,flowcytometry,reversetranscription-polymerasechainreaction(RT-PCR)andWesternblotanalysis.TheresultsshowthatBCNUorATRAshowstime-anddose-dependentinhibitioneffectsonhumanglioblastomaU251cellsandthecombinationofBCNUwithATRAshowsansynergisticinhibitioneffectonhumanglioblastomaU251cells,andthecombinedBCNUandATRAcansignificantlyinhibittheproliferationofhumanglioblastomaU251cells,andinducetheapoptosisofthem,makingthecellsarrestinthestageofG1phase,thestageofSandG2phasesdecline,therateoftheapoptosisofhumanglioblastomaU251cellsincrease,thecorrespondingmRNAexpressionofcyclinEandcyclin-dependentkinase2(CDK2)downregulatedandthecorrespon-dingmRNAexpressionofp27kip1unregulated.Inaddition,thecombinedBCNUandATRAreducedtheproteinexpressionofnuclearfactorkappaB(NF-κB).Takentogether,theseresultssuggestthatthetreatmentofhumanglioblastomaU251cellswithacombinationapplicationofATRAandBCNUcanexertsynergisticeffect,thecourseofthiskindofcombinationchemotherapymaylikelybeassociatedwithmultiplemolecularmechanismsforapoptosis,furthermore,thecyclinEandp27kip1shouldbeconsideredasnoveltargetsforcontrollingthegrowthofglioblastomacells.