Design, Synthesis, Anticancer Activity and Molecular Docking of New 1,2,3-Triazole combined Glucosides with coumarin

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Ruaa Wassim Adam
Ezzat Hussein Zimam


Carbohydrate, 4-hydroxy coumarin, Click chemistery,1,2,3-triazole


The synthetic strategy for the preparation of the targeted glycosides involved two different pathways to obtain two types of hybrid compounds; the first represents new 1,2,3-triazole derivative in the 6-carbon glucopyranose, and the other is a new glycoside of 4-hydroxy coumarin bases. The starting derivative 1 prepared by reaction of 6-azide glucopyranose and 2 ethylene azide-2,3,4,6-tetraacetate- β-D- glucopyranoside with propargyl 4-hydroxy coumarin under click conditions .The cytotoxicity potentials of glucosides derivatives were evaluated by MTT assay against liver cancer primary tissue culture , which appear that derivatives exhibited selective cytotoxicity against liver cancer cells isolated from Iraqi patients with inhibitory concentration (IC50) 106.81 μg/ml. Docking simulation studies were performed to check the binding patterns of the synthesized compounds. Enzyme inhibition assay studies were also conducted for the epidermal growth factor receptor (EGFR), and the results explained the activity of a number of derivatives.

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