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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 shu

Synthesis and Anti-tumor Activities of Arylamino-α-glucofuranose Derivatives

1.
a Key Laboratory of the Ministry of Education for Medicinal Resources and Natural Pharmaceutical Chemistry, School of Chemistry and Chemical Engineering, Shaanxi Normal University, Xi'an 710062, China;
2.
b Chia Tai Tianqing Pharmaceutical Co., Ltd., Nanjing, 210042, China

Corresponding author: LI Baolin,
Received Date: 19 January 2015
Available Online: 17 March 2015
Fund Project: 国家自然科学基金资助项目(21272144) (21272144)

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).
- arylaminogluofuranose derivatives,
- synthesis,
- anti-tumor activity
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