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- W4250941164 abstract "Biological target: The 1,2,3-triazole-linked, diphenyl-substituted neoglycoconjugate 1 is a selective inhibitor of human α-1,3-fucosyltransferase IV (Fuc-T), the enzyme catalysing the final step in the synthesis of oligosaccharides, including the leukocyte and leukaemic cell adhesion molecule, sialyl Lewis X. Therapeutic profile: The compound has potential for the treatment of inflammation and cancer. Synthetic highlights: Neoglycoconjugate 1 is a representative of a GDP-triazole screening library produced by the Cu(I)-catalyzed [2 + 3] cycloaddition reaction between azide and acetylene reactants. It is an example of click chemistry, a modular approach using low-energy chemical transformations to generate collections of test compounds. A more recent extension of click chemistry is target-guided synthesis (TGS) or freeze-frame click chemistry in which a biological target itself is used to assemble inhibitors at the binding site. This represents an exciting new strategy for the generation of compound libraries and the effective selection of hits and leads." @default.
- W4250941164 created "2022-05-12" @default.
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- W4250941164 date "2011-01-01" @default.
- W4250941164 modified "2023-10-18" @default.
- W4250941164 title "Neoglycoconjugate" @default.
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- W4250941164 doi "https://doi.org/10.1007/978-3-0348-0125-6_15" @default.
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