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ID: ALA1147556

Journal: Bioorg Med Chem Lett

Title: Structure-activity relationships of novel inhibitors of glyceraldehyde-3-phosphate dehydrogenase.

Authors: Leitão A, Andricopulo AD, Oliva G, Pupo MT, de Marchi AA, Vieira PC, da Silva MF, Ferreira VF, de Souza MC, Sá MM, Moraes VR, Montanari CA.

Abstract: 3D QSAR studies were performed on a library of 120 GAPDH inhibitors, including a series of coumarins, flavonoids, and nucleosides. The VolSurf method was successfully used to calculate surface descriptors for protein-ligand affinity and binding site of the enzyme. PCA/PLS analyses have permitted the evaluation of the structural features crucial for potency, selectivity, and favorable pharmacokinetic properties, and are important for the design of new ligands.

CiteXplore: 15081008

DOI: 10.1016/j.bmcl.2004.02.025