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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：1559 下载量：312
| 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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