OALib Journal期刊
ISSN: 2333-9721
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新型双氢青蒿素哌嗪-磺酰胺类化合物的合成、结构及生物活性
, PP. 1430-1435
Keywords: 双氢青蒿素,哌嗪衍生物,合成,单晶结构,生物活性
Abstract:
以双氢青蒿素为起始原料,经酯化、胺化、酰化快速、高效地合成了7种新型磺酰胺类双氢青蒿素哌嗪衍生物。通过ir、1hnmr、13cnmr和hr-ms对所有化合物进行了结构确定。并用x-单晶衍射法对化合物3c进行了最终构型确证。同时,以cck-8法对部分化合物进行了体外hela细胞毒性测试,初步测试结果表明:目标化合物对hela细胞有明显的抑制细胞增殖、诱导其凋亡的细胞毒活性,ic50最优值为0.14μmol·l-1。
References
[1] | lees.artemisinin,promisingleadnaturalproductforvariousdrugdevelopments[j].minirevmedchem,2007,7:411-422.
|
[2] | chenh,sunb,pans,etal.dihydroartemisinininhibitsgrowthofpancreaticcancercellsinvitroandinvivo[j].anticancerdrugs,2009,20:131-140.
|
[3] | wanzk,chenaile,lihq,etal.discoveryofhsd-621asapotentialagentforthetreatmentoftype2diabetes[j].jmedchemlett,2013,4:118-121.
|
[4] | pfefferkornja,guzman-pereza,litchfieldj,etal.discoveryof(s)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1h-imidazol-1-yl)propanamido)nicotinicacidasahepatoselectiveglucokinaseactivatorclinicalcandidatefortreatingtype2diabetesmellitus[j].jmedchem,2012,55:1318-1333.
|
[5] | borrmannt,hinzs,bertarellidc,etal.1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines:developmentandcharacterizationofadenosinea2breceptorantagonistsandanewradioligandwithsubnanomolaraffinityandsubtypespecificity[j].jmedchem,2009,52:3994-4006.
|
[6] | huangsx,lihy,liujy,etal.incorporationofpiperazinofunctionalityinto1,3-disubstitutedureaasthetertiarypharmacophoreaffordingpotentinhibitorsofsolubleepoxidehydrolasewithimprovedpharmacokineticproperties[j].jmedchem,2010,53:8376-8386.
|
[7] | liun,yanglh,zhangzx,etal.studiesontheconversitionofepimersofdihydroartemisinin[j].chinjpharmanal(药物分析杂志),2002,22:303.
|
[8] | lij,zhouhj.dihydroartemisinininhibitstheexpressionofvascularendothelialgrowthfactorink562cells[j].actapharmsin(药学学报),2005,40:1041-1045.
|
[9] | chenhh,zhouhj.inhibitoryeffectsofartesunateonangiogenesis[j].actapharmsin(药学学报),2004,39:29-33.
|
[10] | fengts,guantaiem,nellmj,etal.antiplasmodialandantitumoractivityofdihydroartemisininanalogsderivedviatheaza-michaeladditionreaction[j].bioorgmedchemlett,2011,21:2882-2886.
|
[11] | chenwq,qihw,wucg,etal.effectofdihydroartemisininonproliferationofhumanlungadenocarcinomacelllinea549[j].chinalungcancer(中国肺癌杂志),2005,8:85-88.
|
[12] | singhnp,laih.selectivetoxicityofdihydroartemisininandholotransferrintowardhumanbreastcancercells[j].lifesci,2001,70:b49-56.
|
[13] | jiaoy,gecm,mengqh,etal.dihydroartemisininisaninhibitorofovariancancercellgrowth[j].actapharmacolsin,2007,28:1045-1056.
|
[14] | genoveserf,newmandb.understandingartemisinin-inducedbrainstemneurotoxicity[j].archtoxicol,2008,82:379-385.
|
[15] | chos,ohs,umy,etal.synthesisof10-substitutedtriazolylartemisininspossessinganticanceractivityviahuisgen1,3-dipolarcylcoadition[j].bioorgmedchemlett,2009,19:382-385.
|
[16] | hindleys,wardsa,storrrc,etal.mechanism-baseddesignofparasite-targetedartemisininderivatives:synthesisandantimalarialactivityofnewdiaminecontaininganalogues[j].jmedchem,2002,45:1052-1063.
|
[17] | pacorelb,leungsc,stachulskiav,etal.modularsynthesisandinvitroandinvivoantimalarialassessmentofc-10pyrrolemannichbasederivativesofartemisinin[j].jmedchem,2010,53:633-640.
|
[18] | hey,mawy,zhangcn.synthesisandactivitiesof4-deoxy-4β-arylmethylenesulfonylamido-4'-demethylpodophyllotoxins[j].actapharmsin(药学学报),2001,36:105-107.
|
[19] | songhb,caosl,zhengxl.advancesinsulfonamidesasantitumoragents[j].chinjnewdrugs(中国新药杂志),2009,18:108-115.
|
[20] | bergs,berghm,hellbergs,etal.discoveryofnovelpotentandhighlyselectiveglycogensynthasekinase-3β(gsk3β)inhibitorsforalzheimer'sdisease:design,synthesis,andcharacterizationofpyrazines[j].jmedchem,2012,55:9107-9119.
|
[21] | houcm,lixy,xip,etal.thecomparisonofmttandcck-8cellproliferationassaysuspension[j].bullacadmilmedsci(军事医学科学院院刊),2009,33:400-401.
|
[22] | sunj,meij,zhaoxh,etal.effectsofbioactiveplantcomponentsoncellviabilityandcomparisonofcellviableassays[j].foodsci(食品科学),2012,33:119-123.
|
[23] | jiangw,zhangy,xiaol,etal.cannabinoidspromoteembryonicandadulthippocampusneurogenesisandproduceanxiolytic-andantidepressant-likeeffects[j].jclininvest,2005,115:3104-3116.
|
[24] | gongxm,zhouda,caojp,etal.cytotoxiceffectandradiationenhancementofartemisinininuterinecervicalcarcinomacelllinehela[j].suzhouunivjmedsci(苏州大学学报医学版),2010,30:224-226.
|
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