引用本文:
孙宝丽, 张娅玲, 王丽丽, 张喜全, 顾红梅, 李宝林. 芳氨基代-α-呋喃葡萄糖衍生物的合成及抗肿瘤活性[J]. 应用化学,
2015, 32(9): 987-993.
doi:
10.11944/j.issn.1000-0518.2015.09.150019
Citation: SUN Baoli, ZHANG Yaling, WANG Lili, ZHANG Xiquan, GU Hongmei, LI Baolin. Synthesis and Anti-tumor Activities of Arylamino-α-glucofuranose Derivatives[J]. Chinese Journal of Applied Chemistry, 2015, 32(9): 987-993. doi: 10.11944/j.issn.1000-0518.2015.09.150019
Citation: SUN Baoli, ZHANG Yaling, WANG Lili, ZHANG Xiquan, GU Hongmei, LI Baolin. Synthesis and Anti-tumor Activities of Arylamino-α-glucofuranose Derivatives[J]. Chinese Journal of Applied Chemistry, 2015, 32(9): 987-993. doi: 10.11944/j.issn.1000-0518.2015.09.150019
芳氨基代-α-呋喃葡萄糖衍生物的合成及抗肿瘤活性
摘要:
分别以2-甲基-5-硝基苯甲酸、2-氯-5-硝基苯甲酸为原料,经羧基氯化、Friedel-Crafts酰基化、羰基还原、硝基还原和还原胺化反应合成了4种新型的1,2-O-异丙叉基-5-芳氨基代-α-呋喃葡萄糖衍生物。利用IR、NMR和HRMS等技术手段对反应所及中间体及目标化合物进行了结构测定和表征,并采用MTT法将目标化合物对3种人体肿瘤细胞的抗肿瘤活性进行了初步评价。结果表明,目标化合物1a1对肿瘤细胞的生长抑制作用优于其它3种目标化合物,特别是对A431细胞表现出更明显的生长抑制活性(IC50:(6.54±1.34)μmol/L)。
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关键词:
- 芳氨基代葡萄糖衍生物
- / 合成
- / 抗肿瘤活性
English
Synthesis and Anti-tumor Activities of Arylamino-α-glucofuranose Derivatives
Abstract:
Four novel 1,2-O-isopropylidene-5-arylamino-α-glucofuranose derivatives were prepared using2-methyl-5-nitrobenzoicacid and 2-chloro-5-nitrobenzoic acid,respectively,as the starting materials by a synthetic route including chlorination of carboxylic acid,Friedel-Crafts acylation,reduction of carbonyl,reduction of nitro and reductive amination.The structures of intermediates and target compounds were characterized by IR,NMR and HRMS.The anti-tumor activities of target compounds on three kinds of cells were tested preliminarily by MTT method.The results indicate that the anti-tumor activitives of compound 1a1 is better than other three kinds of target compounds on three kinds of tumor cells,especially on A431(IC50:(6.54±1.34)μmol/L).
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Key words:
- arylaminogluofuranose derivatives
- / synthesis
- / anti-tumor activity
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