Studies on the Synthesis,the 2D and 3D—QSAR About Lipophilic Antifolate 2,4—Diamino—5—methyl—6—(Substituted Benzylamino)Quinazoline Compounds

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摘要 Methetraxate(MTX),aclassicaldihydrofolatereductaseinhibitor,wasasuccessfulclinicalantitumoragent,havingpotentinhibitoryactivitiestoseveralkindsoftumors.Unfortunately,thecancercellkswereeasiertoproduceresistancetoMTXwhichendedinthefailureofchemotherapy.Inordertoovercometheresistanceoftumorcells,anewkindofdihydrofolatereductaseinhibitorscallednonclassicalantifolateincludingtriazines,pyrimidinesandquinazolinesweredesignedandsynthesized.Becauseofthedifferentantitumormechanismsbetweenthetwokindsofcompunds,thecancercellsresistanttoMTXmaystillbesensitivetothenonclassicalantifolate.Accordingtothistheory,somenonclassicalantifolate2,4-diamino-5-methyl-6-(substitutedbenzylamino)quinazolineswiththegeneralstructureshowninFIg.1weresynthesizedandtheirantitumoractivitiesweredeterminedinthisthesis.
机构地区 不详
出处 《中国药学:英文版》 1997年2期
出版日期 1997年02月12日(中国期刊网平台首次上网日期,不代表论文的发表时间)
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