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新型双β-咔啉碱的设计、合成与抗肿瘤活性研究

发表时间:2013-04-15  浏览量:1330  下载量:258
全部作者: 马芹,施步席,范文玺,郭亮,白著双,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: 目的:设计新型双β-咔啉碱并评价其抗肿瘤活性。方法:以L-色氨酸为原料,经Spictet-Spengler缩合、酯化、氧化、烷基化等5步反应合成了6个新型双β-咔啉碱,采用噻唑蓝(MTT)法和6种人肿瘤细胞系对目标化合物进行了体外抗肿瘤活性评价。结果:所有目标化合物的结构经FAB-MS,1H NMR和13C NMR 进行了结构确认。体外抗肿瘤活性测试结果表明,桥链长度为6个亚甲基的双β-咔啉碱6c具有最好的抗肿瘤活性,所有目标化合物对KB细胞系具有选择的抗肿瘤活性。结论:这类化合物具有开发成抗肿瘤创新药物的潜力。
关 键 词: 有机化学;合成;双β-咔啉碱;抗肿瘤
Title: Study on the design, synthesis and antitumor activity of novel bivalent β-carbolines
Author: MA Qin, SHI Buxi, FAN Wenxi, GUO Liang, BAI Zhushuang, CAO Rihui
Organization: Xinjiang Huashidan Pharmaceutical Research Co., Ltd.; School of Chemistry and Chemistry Engineering, Sun Yat-sen University
Abstract: Objective: To design novel bivalent β-carbolines and evaluate its antitumor activities. Methods: Six novel bivalent β-carbolines was synthesized from the starting material L-tryptophan by Spictet-Splengler condensation, esterification, oxidation and alkylation. The antitumor activities of all bivalent β-carbolines were evaluated in vitro through against a panel of human tumor cell lines and using the mothod of MTT. Results: The chemical structures of all the newly synthesized compounds were characterized by FAB-MS,1H NMR and 13C NMR. The experiment of in vitro antitumor activities demonstrated that compound 6c with a spacer of six methylene units exhibited the best antitumor activity, and all bivalent β-carbolines had selective antitumor activities against KB cell lines. Conclusion: These compounds might be a novel promising class of antitumor agents with clinical development potential.
Key words: organic chemistry; synthesis; bivalent β-carbolines; antitumor
发表期数: 2013年4月第7期
引用格式: 马芹,施步席,范文玺,等. 新型双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,2013,6(7):655-660.
 
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