72691-30-6Relevant academic research and scientific papers
Aldolase-catalyzed synthesis of β-D-Galp-(1→9)-D-KDN: A novel acceptor for sialyltransferases
Yu, Hai,Chen, Xi
, p. 2393 - 2396 (2006)
β-D-Galp-(1→9)-D-KDN, a disaccharide component of the cell wall of Streptomyces sp. MB-8, was synthesized from β-D-Galp-(1→6)-D-Manp and pyruvate using a sialic acid aldolase. The obtained KDN-containing compound was a novel acceptor for bacterial sialylt
Design, synthesis, and biological evaluation of novel carbohydrate-based sulfamates as carbonic anhydrase inhibitors
Lopez, Marie,Trajkovic, Jonathan,Bornaghi, Laurent F.,Innocenti, Alessio,Vullo, Daniela,Supuran, Claudiu T.,Poulsen, Sally-Ann
supporting information; experimental part, p. 1481 - 1489 (2011/05/12)
Carbonic anhydrases (CAs) IX and XII are enzymes with newly validated potential for the development of personalized, first-in-class cancer chemotherapies. Here we present the design and synthesis of novel carbohydrate-based CA inhibitors, several of which were very efficient inhibitors (Ki10 nM) with good selectivity for cancer-associated CA isozymes over off-target CA isozymes. All inhibitors comprised a carbohydrate core with one hydroxyl group derivatized as a sulfamate. Five different carbohydrates were chosen to present a selection of molecular shapes with subtle stereochemical differences to the CA enzymes active site. Variable modifications of the remaining sugar hydroxyl groups were incorporated to provide an incremental coverage of chemical property parameters that are associated with biopharmaceutical performance. All sulfamate inhibitors displayed ligand efficiencies that are consistent with those reported for good drug lead candidates.
