Nicotinamide phosphoribosyltransferase inhibitors, design, preparation, and structure–activity relationship

…, J Tjørnelund, P Fristrup, A Thougaard…

Index: Christensen, Mette K.; Erichsen, Kamille D.; Olesen, Uffe H.; Tjornelund, Jette; Fristrup, Peter; Thougaard, Annemette; Nielsen, Soren Jensby; Sehested, Maxwell; Jensen, Peter B.; Loza, Einars; Kalvinsh, Ivars; Garten, Antje; Kiess, Wieland; Bjoerkling, Fredrik Journal of Medicinal Chemistry, 2013 , vol. 56, # 22 p. 9071 - 9088

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Citation Number: 16

Abstract

Existing pharmacological inhibitors for nicotinamide phosphoribosyltransferase (NAMPT) are promising therapeutics for treating cancer. By using medicinal and computational chemistry methods, the structure–activity relationship for novel classes of NAMPT inhibitors is described, and the compounds are optimized. Compounds are designed inspired by the NAMPT inhibitor APO866 and cyanoguanidine inhibitor scaffolds. In comparison with ...