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期刊文章详细信息

苯甲酸氮芥衍生物的合成及抗肿瘤活性    

Synthesis and antitumor activity of benzoic nitrogen mustard derivatives

  

文献类型:期刊文章

作  者:罗稳[1] 赵永梅[1] 王玉霞[1] 谢松强[2] 赵瑾[1] 王超杰[1]

机构地区:[1]河南大学化学化工学院天然产物研究所,河南开封475001 [2]河南大学药学院,河南开封475001

出  处:《药学学报》

基  金:河南省科技攻关项目(496410030);河南大学重点学科资助项目.

年  份:2007

卷  号:42

期  号:12

起止页码:1327-1329

语  种:中文

收录情况:AJ、BDHX、BDHX2004、BIOSISPREVIEWS、CAB、CAS、CSCD、CSCD2011_2012、DOAJ、EMBASE、IC、IPA、JST、PUBMED、RCCSE、RSC、SCOPUS、WOS、ZGKJHX、核心刊

摘  要:To study the effect of isoprenoid and aliphatic saturated alcohols as modificator on benzoic nitrogen mustard,the intermediate 4-[N,N-bis(2-chloroethyl)amino] benzoic acid 4 was prepared in four steps utilizing p-amino benzoic acid as the starting material.Target compounds were synthesized by the catalytic esterification of DCC/DMAP and the structures of the six new esters were characterized by elemental analysis,1H NMR,13C NMR and MS.Antitumor activities were evaluated in vitro using MTT assay.The result showed that some derivatives were more potent than the intermediate 4,and compound 5c modified with dodecanol exhibited similar activity to the commercial drug melphalan.

关 键 词:苯甲酸氮芥  合成  抗肿瘤

分 类 号:R916.2[药学类]

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