SAR and characterization of non-substrate isoindoline urea inhibitors of nicotinamide phosphoribosyltransferase (NAMPT)

[Display omitted] Herein we disclose SAR studies that led to a series of isoindoline ureas which we recently reported were first-in-class, non-substrate nicotinamide phosphoribosyltransferase (NAMPT) inhibitors. Modification of the isoindoline and/or the terminal functionality of screening hit 5 pro...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2017-08, Vol.27 (15), p.3317-3325
Hauptverfasser:	Curtin, Michael L., Heyman, H. Robin, Clark, Richard F., Sorensen, Bryan K., Doherty, George A., Hansen, T. Matthew, Frey, Robin R., Sarris, Kathy A., Aguirre, Ana L., Shrestha, Anurupa, Tu, Noah, Woller, Kevin, Pliushchev, Marina A., Sweis, Ramzi F., Cheng, Min, Wilsbacher, Julie L., Kovar, Peter J., Guo, Jun, Cheng, Dong, Longenecker, Kenton L., Raich, Diana, Korepanova, Alla V., Soni, Nirupama B., Algire, Mikkel A., Richardson, Paul L., Marin, Violeta L., Badagnani, Ilaria, Vasudevan, Anil, Buchanan, F. Greg, Maag, David, Chiang, Gary G., Tse, Chris, Michaelides, Michael R.
Format:	Artikel
Sprache:	eng
Schlagworte:	60 APPLIED LIFE SCIENCES Animals Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacokinetics Antineoplastic Agents - pharmacology Antineoplastic Agents - therapeutic use Antitumor activity BASIC BIOLOGICAL SCIENCES Cancer Cell Line, Tumor Cell Proliferation - drug effects Crystallography, X-Ray Cytokines - antagonists & inhibitors Cytokines - chemistry Cytokines - metabolism Drug Discovery Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacokinetics Enzyme Inhibitors - pharmacology Enzyme Inhibitors - therapeutic use Humans Isoindoles - chemistry Isoindoles - pharmacokinetics Isoindoles - pharmacology Isoindoles - therapeutic use Isoindoline ureas Mice Models, Molecular NAMPT inhibitors Neoplasms - drug therapy Neoplasms - metabolism Neoplasms - pathology Nicotinamide Phosphoribosyltransferase - antagonists & inhibitors Nicotinamide Phosphoribosyltransferase - chemistry Nicotinamide Phosphoribosyltransferase - metabolism Structure-Activity Relationship Urea - analogs & derivatives Urea - pharmacokinetics Urea - pharmacology Urea - therapeutic use
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