105356-51-2Relevant academic research and scientific papers
The identification and optimization of 2,4-diketobutyric acids as flap endonuclease 1 inhibitors
Tumey, L. Nathan,Huck, Bayard,Gleason, Elizabeth,Wang, Jianmin,Silver, Daniel,Brunden, Kurt,Boozer, Sherry,Rundlett, Stephen,Sherf, Bruce,Murphy, Steven,Bailey, Andrew,Dent, Tom,Leventhal, Christina,Harrington, John,Bennani, Youssef L.
, p. 4915 - 4918 (2007/10/03)
Flap endonuclease 1 (FEN1) is a key enzyme involved in base excision repair (BER), a primary pathway utilized by mammalian cells to repair DNA damage. In this report, we describe the identification and SAR of a series of 2,4-diketobutyric acid FEN1 inhibi
Discovery of α,γ-Diketo Acids as Potent Selective and Reversible Inhibitors of Hepatitis C Virus NS5b RNA-Dependent RNA Polymerase
Summa, Vincenzo,Petrocchi, Alessia,Pace, Paola,Matassa, Victor G.,De Francesco, Raffaele,Altamura, Sergio,Tomei, Licia,Koch, Uwe,Neuner, Philippe
, p. 14 - 17 (2007/10/03)
α,γ-Diketo acids (DKA) were discovered from screening as selective and reversible inhibitors of hepatitis C virus NS5b RNA-dependent RNA polymerase. The diketo acid moiety proved essential for activity, while substitution on the γ position was necessary for selectivity and potency. Optimization led to the identification of a DKA inhibitor of NS5b polymerase with IC50 = 45 nM, one of the most potent HCV NS5b polymerase inhibitors reported.
