1067243-69-9Relevant academic research and scientific papers
Functionalized pyrrolidine inhibitors of human type II α-mannosidases as anti-cancer agents: Optimizing the fit to the active site
Fiaux, Helene,Kuntz, Douglas A.,Hoffman, Daniela,Janzer, Robert C.,Gerber-Lemaire, Sandrine,Rose, David R.,Juillerat-Jeanneret, Lucienne
, p. 7337 - 7346 (2008)
Refining the chemical structure of functionalized pyrrolidine-based inhibitors of Golgi α-mannosidase II (GMII) to optimize binding affinity provided a lead molecule that demonstrated nanomolar competitive inhibition of α-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.
