Direct Semi-Synthesis of the Anticancer Lead-Drug Protoapigenone from Apigenin, and Synthesis of Further New Cytotoxic Protoflavone Derivatives 英文参考文献.docVIP

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Direct Semi-Synthesis of the Anticancer Lead-Drug Protoapigenone from Apigenin, and Synthesis of Further New Cytotoxic Protoflavone Derivatives 英文参考文献.doc

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Direct Semi-Synthesis of the Anticancer Lead-Drug Protoapigenone from Apigenin, and Synthesis of Further New Cytotoxic Protoflavone Derivatives 英文参考文献

DirectSemi-SynthesisoftheAnticancerLead-Drug ProtoapigenonefromApigenin,andSynthesisofFurther NewCytotoxicProtoflavoneDerivatives AttilaHunyadi1,2.,Da-WeiChuang2.,BalazsDanko1,MichaelY.Chiang3,Chia-LinLee4 ,Hui-Chun Wang2,Chin-ChungWu2,Fang-RongChang2,5,6*,Yang-ChangWu2,4,7 * 1Institute of Pharmacognosy, University of Szeged, Szeged, Hungary, 2Graduate Institute of Natural Products, Kaohsiung Medical University, Kaohsiung, Taiwan, 3DepartmentofChemistry,NationalSunYat-SenUniversity,Kaohsiung,Taiwan,4GraduateInstituteofIntegratedMedicine,CollegeofChineseMedicine,ChinaMedical University, Taichung, Taiwan, 5Cancer Center, Kaohsiung Medical University Hospital, Kaohsiung, Taiwan, 6Research and Development Center of Chinese Herbal Medicines and New Drugs, College of Pharmacy, Kaohsiung Medical University, Kaohsiung, Taiwan, 7Natural Medicinal Products Research Center, China Medical UniversityHospital,Taichung,Taiwan Abstract Protoapigenone,anaturalflavonoidpossessinganunusualp-quinolmoietyonitsB-ring,isanovelprospectiveanticancer agentwithlowtoxicitythatiscurrentlyindevelopment.Thefirsteconomical,one-stepsynthesisofprotoapigenonefrom apigeninisdescribedonuptogramscale.13new19-O-alkylflavoneanalogswerealsosynthesized,eitherfromapigeninor b-naphthoflavone. The in vitro cytotoxic activity of each compound was tested on six human cancer cell lines (HepG2, Hep3B, Ca9-22, A549, MCF-7 and MDA-MB-231). In the case of 19-O-alkyl-protoapigenone derivatives, structure-activity relationships were found depending on the side-chain, and protoapigenone 19-O-butyl ether was found to exert significantly stronger activity against three of the cell lines (Hep3B, MCF-7 and MDA-MB-231) than its non-substituted analog, protoapigenone itself. In contrast to this, all b-naphthoflavone derivatives bearing the same pharmacophore on theirB-ringshoweddecreasedcytotoxicactivitieswhensubstitutedwithanO-alkylside-chainatposition19,comparingto thatofthenon-substitutedcompound. Citation:HunyadiA,Chuan