Article: article from journal or magazin.
Functionalized pyrrolidine inhibitors of human type II alpha-mannosidases as anti-cancer agents: optimizing the fit to the active site.
Bioorganic & [and] Medicinal Chemistry
Refining the chemical structure of functionalized pyrrolidine-based inhibitors of Golgi alpha-mannosidase II (GMII) to optimize binding affinity provided a lead molecule that demonstrated nanomolar competitive inhibition of alpha-mannosidases II and an optimal fit in the active site of Drosophila GMII by X-ray crystallography. Esters of this lead compound also inhibited the growth of human glioblastoma and brain-derived endothelial cells more than the growth of non-tumoral human fibroblasts, suggesting their potential for anti-cancer therapy.
Animals, Antineoplastic Agents, Binding Sites, Cell Line, Tumor, Drosophila, Endothelial Cells, Fabaceae, Glioblastoma, Humans, Models, Molecular, Molecular Structure, Pyrrolidines, Structure-Activity Relationship, alpha-Mannosidase
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