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新型烷氨基桥连双β-咔啉碱的设计合成与抗肿瘤活性研究

发表时间:2015-02-15  浏览量:1412  下载量:602
全部作者: 马芹,张国贤,范文玺,郭亮,李键茹,曹日晖
作者单位: 新疆华世丹药物研究有限责任公司;中山大学化学与化学工程学院
摘 要: 以L-色氨酸为原料,经Spictet-Spengler缩合、氧化脱酸、烷基化、氧化、缩合并还原等5步反应合成4个新型水溶性双β-咔啉碱,采用噻唑蓝(thiazolyl blue,MTT)法和10种人肿瘤细胞系对目标化合物进行体外抗肿瘤活性评价。所有目标化合物的结构经电喷雾质谱(electrospray ionization mass spectrometry,ESI-MS),1H NMR,13C NMR,高分辨率质谱(high resolution mass spectrometry, HRMS)进行结构确认。体外抗肿瘤活性测试结果表明,烷氨基桥连双β-咔啉碱具有良好的水溶解性,长度为5个亚甲基的双β-咔啉碱具有最佳的抗肿瘤活性。
关 键 词: 有机化学;合成;双β-咔啉碱;抗肿瘤
Title: Design, synthesis and antitumor activities of novel bivalentβ-carbolines linked by alkylamino spacer
Author: MA Qin, ZHANG Guoxian, FAN Wenxi, GUO Liang, LI Jianru, CAO Rihui
Organization: Xinjiang Huashidan Pharmaceutical Research Co. Ltd., School of Chemistry and Chemical Engineering, Sun Yat-sen University
Abstract: Four novel bivalent β-carbolines with a spacer of three to six methylene units between the 3-methylamino group were synthesized from the starting material L-tryptophan by Spictet-Splengler condensation, oxidative decarboxylation, alkylation, oxidation, condensation and reduction. All compounds were evaluated against ten human tumor cell lines using thiazolyl blue (MTT) method. The chemical structures of all the newly synthesized compounds were characterized by electrosprany inonization mass spectrometry (ESI-MS), 1H NMR, 13C NMR and high resolution mass spectnometry(HRMS). The cytotoxic activities of all bivalent β-carbolines was evaluated in vitro against a panel of human tumor cell lines and compared with the reference drugs cisplatin. The results demonstrated that compound with a spacer of five methylene units exhibited more potent cytotoxic activities.
Key words: organic chemistry; synthesis; bivalent β-carbolines; antitumor
发表期数: 2015年2月第3期
引用格式: 马芹,张国贤,范文玺,等. 新型烷氨基桥连双β-咔啉碱的设计合成与抗肿瘤活性研究 [J]. 中国科技论文在线精品论文,2015,8(3):222-228.
 
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