Ward, Richard A.; Brassington, Claire; Breeze, Alexander L.; Caputo, Alessandro; Critchlow, Susan; Davies, Gareth; Goodwin, Louise; Hassall, Giles; Greenwood, Ryan; Holdgate, Geoffrey A.; Mrosek, Michael; Norman, Richard A.; Pearson, Stuart; Tart, Jonathan; Tucker, Julie A.; Vogtherr, Martin; Whittaker, David; Wingfield, Jonathan; Winter, Jon; Hudson, Kevin published the artcile< Design and Synthesis of Novel Lactate Dehydrogenase A Inhibitors by Fragment-Based Lead Generation>, Electric Literature of 606-68-8, the main research area is lactate dehydrogenase A inhibitor preparation lead generation SAR.
Lactate dehydrogenase A (LDHA) catalyzes the conversion of pyruvate to lactate, utilizing NADH as a cofactor. It has been identified as a potential therapeutic target in the area of cancer metabolism In this manuscript we report our progress using fragment-based lead generation (FBLG), assisted by x-ray crystallog. to develop small mol. LDHA inhibitors. Fragment hits were identified through NMR and SPR screening and optimized into lead compounds with nanomolar binding affinities via fragment linking. Also reported is their modification into cellular active compounds suitable for target validation work.
Journal of Medicinal Chemistry published new progress about Antitumor agents. 606-68-8 belongs to class chiral-phosphine-ligands, and the molecular formula is C21H27N7Na2O14P2, Electric Literature of 606-68-8.
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Phosphine ligand,
Chiral phosphine ligands in asymmetric synthesis. Molecular structure and absolute configuration of (1,5-cyclooctadiene)-(2S,3S)-2,3-bis(diphenylphosphino)butanerhodium(I) perchlorate tetrahydrofuran solvate