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᩾ጛ ʘ͍ିᜑϣĭՈȌtǎûྃӨϏɳۘऺ (ˤάϒŻ(˳Ŀሳ̓ƚሳƚ┦ሳĭĚƚνۘǘǩ*310053Η ĺ1,2,3,4-ʕDZ-β-ƳȐ-3->Ɋ!īϗˤα-ƳȐ;β-ƳȐʼᡅֲՈţɶƳȐ̼͙ÖĢǰʢ<ʷ°Ŋɺǜ<5ͩ ΢Ǝ͊ƭĽijƒ–ƙ™6-ŀα-ƳȐ̼;6-ŀβ-ƳȐ̼ĺ3-ŀβ-ƳȐ̼͙ÖˤØMTTɉ]RƋÝèţZ° 1 ŊΙÁũʲ›ZØ<඗ȘţɶC15ϣũƳȐ̼͙ÖˤΦ¥΢ƎHNMRƮESI-MSȗ<඗᩾MTTɉʅʍ ƙũƋÝèţZ2ɷŁΙÁìˀ=m^/ũʷ°Ŋɺǜˤșƒèţ4ɇzΉǜZιͫ‰ɐƐŶɺeũ°ŊΙ Áʲ›ɺǜ< ͟⏲᪑ƳȐ͙Ö˳ţɶ˳ʷ°Ŋɺǜ Aতේǻ1007-7693(2013)03-0229-06ۅିǻR916.696Dzʃȣ Ě SynthesisandAntitumorActivityStudyofCarbolineDerivatives CHENJing,TAOXuefeng(DepartmentofMedicinalChemistry,CollegeofPharmaceuticalScience,ZhejiangChinese MedicinalUniversity,Hangzhou310053,China) ABSTRACT:OBJECTIVETosynthesizeaseriesofcarbolinederivativesanddeterminetheirantitumoractivity. METHODS6-Substituted-α-carbolinederivatives,6-substituted-β-carbolinederivativesand3-substituted-β-carboline derivativesweresynthesizedthroughseveralstepsfromα-carboline,β-carbolineand1,2,3,4-tetrahydro-β-carboline-3-carboxylic acidseparately.TheantitumoractivitiesofthetargetcompoundswerestudiedbyMTTmethod.RESULTSFifteennovel 1 carbolinederivativesweresynthesizedandtheirstructureswerecharacterizedbyHNMRandESI-MS.CONCLUSIONAll thetargetcompoundsshowedantitumoractivityagainstthetestedtumorcells,somewerecomparablewiththatoftaxol. KEYWORDS:carbolinederivatives;synthesis;antitumoractivity ʘ͍ିĚȌĭ«PିËͯ OzႮϢАͣƅÏα-ʘ͍ିᜑϣĭ(8)36-ǚÏ-β-ʘ͍ିᜑϣĭ(9) ,&Yɳ඗ȀՈϣĭݵͣƅûነ3û҉ɦ3ûྃӨ3Ñǎ3-ǚÏ-β-ʘ͍ିᜑϣĭ(17)͝15ţ ûᜄʏÑǎȞࠢඓிඣõ:਍Ϗɳ[1-5]4͢ĚȌĭ&᪩ିĚȌĭՈẟPǹ᪂ᩥŌǕȴƇr Ө᫵Ë਍ĄͥǛ4r¦ØՈËͯ͟ͼ4ƨ᫂Lඈ᪩ିĚȌĭńûྃӨ5☦ϵzͣƅ̶☺ͥ3ûȖ܄4 X R ńQƛ1ňÑγ-ʘ͍&ɡʴ᪂ᩥ3Ȍtr52 [6-8] γ-(11) ିRƅ]ȐƓ⏂Ոʘ͍ିᜑϣĭĚ4N !ǹՈûྃӨϏɳϟ᪙ᜬŠ̓ᾬ ĚȌĭͣƅËN R ᫵ՈûྃӨϏɳaᾬ ĚȌĭՈϏɳ^⓷ɳȭ1 1 :X=NHSO2orSO2NHorSO3orNHCOorCO ௯Dž⁋ּƟ4ûྃӨňϬƶ:ǒɀº߾᪩ି+ ĚȌĭţỞẋõ:Ǻ੥ᖏՁ༞Ȍzȶ͑DNAݵȖĚ1γ-çĘśέÛʦ(1)ĝ̼͸Bʊ Fig1Structureofγ-carbolinederivatives(1) ȭǕƉûྃӨňϬ4ƨÑQƛȌtՈγ-ʘ͍ ିᜑϣĭ&̴ȰĚȌĭljН͢ϏɳṇʌՈƓ1Ȍtǒɀ ⏂ċɉ(϶ʻȖ3Ũ௤ǚÏՈᆳɳ޾‴྾Ȗ3‴1.1ք^᪙F ྾ȖẢȉ⏂)໇ȓʘ͍ɡʴᆳɳZNƣƄĹาՈBrukerAM400Ƨʴޅ͝ƓÖ(ȃęBruker͘ ǜĚȭ᪩ିĚȌĭϏɳՈƽˑ4Ȍtǣ4r6-ǚǼ)Esquire-LC-00075^ᯬ༘ϬÖ(ȃęBruker͘ (Ȗₕ-ֲęǪႮϢ࢕ƚȖₕ-ֲ(81102315)ʌ਍ƚʝŞ̇ƚ࢕ͥc-࢕ۘȖₕ(20103322120002 ň້੄·┌☝ΏŞ̇᩶TTel:(0571)86613657E-mail:cjmaggie@163.com ęɴÏàϬሳƚ2013