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Novel pyrrolidine 3,4-diol derivatives of the type (2R and 2S,3R,45){[(( 1R)-1-methoxycarbonyl and hydroxylmethyl)-1-arylmethyl)amino] ethyl}-pyrrolidine-3,4-diol have been prepared and evaluated as a-mannosidase inhibitors and assayed for their anticancer activity in vitro. They all exhibit specific but moderate activity as inhibitors towards a-mannosidase from Jack beans. Compounds 7 and 8b bearing hydroxymethyl and trifluoromethylbiphenyl groups show the best antiproliferative effect in two pancreatic cancer cell lines.
Douglas Hanahan, Krisztian Homicsko, Mohammad Sadegh Saghafinia, Stephan Wullschleger, Iacovos Michael, Giovanni Ciriello