The identification and optimization of 2,4-diketobutyric acids as flap endonuclease 1 inhibitors

  • Bioorg Med Chem Lett. 2004 Oct 4;14(19):4915-8. doi: 10.1016/j.bmcl.2004.07.028.
L Nathan Tumey  1 ,  Bayard Huck ,  Elizabeth Gleason ,  Jianmin Wang ,  Daniel Silver ,  Kurt Brunden ,  Sherry Boozer ,  Stephen Rundlett ,  Bruce Sherf ,  Steven Murphy ,  Andrew Bailey ,  Tom Dent ,  Christina Leventhal ,  John Harrington ,  Youssef L Bennani
Affiliations
PMID: 15341951 DOI: 10.1016/j.bmcl.2004.07.028
Abstract

There have been several recent reports of chemopotentiation via inhibition of DNA repair processes. 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 inhibitors.

Products