Design, Synthesis, and Pharmacological Evaluation of Fluorinated Tetrahydrouridine Derivatives as Inhibitors of Cytidine Deaminase

Several 2′-fluorinated tetrahydrouridine derivatives were synthesized as inhibitors of cytidine deaminase (CDA). (4R)-2′-Deoxy-2′,2′-difluoro-3,4,5,6-tetrahydrouridine (7a) showed enhanced acid stability over tetrahydrouridine (THU) 5 at its N-glycosyl bond. As a result, compound 7a showed an improv...

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Veröffentlicht in:	Journal of medicinal chemistry 2014-03, Vol.57 (6), p.2582-2588
Hauptverfasser:	Ferraris, Dana, Duvall, Bridget, Delahanty, Greg, Mistry, Bipin, Alt, Jesse, Rojas, Camilo, Rowbottom, Christopher, Sanders, Kristen, Schuck, Edgar, Huang, Kuan-Chun, Redkar, Sanjeev, Slusher, Barbara B, Tsukamoto, Takashi
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Azacitidine - analogs & derivatives Azacitidine - pharmacology Biological Availability Cytidine Deaminase - antagonists & inhibitors Drug Design Drug Stability Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - pharmacokinetics Enzyme Inhibitors - pharmacology Excitatory Postsynaptic Potentials Fluorine Gastric Juice - chemistry Macaca mulatta Models, Molecular Molecular Conformation Structure-Activity Relationship Tetrahydrouridine - analogs & derivatives Tetrahydrouridine - chemical synthesis Tetrahydrouridine - pharmacology
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