8]naphthyridin-6(5H)-one

Description

XU1 is a potent and selective pan Aurora inhibitor; Phosphorylation of histone H3 (pHH3) inhibitor.

Uses

Benzo[c][1,8]naphthyridin-6(5H)-one exhibits low micromolar affinity to human adenosine receptor (AR) A1 and hA2A, with Ki of 4.6 and 4.8 μM. Benzo[c][1,8]naphthyridin-6(5H)-one is inhibitor for poly ADP-ribose polymerase-1 (PARP-1) and aurora kinase A, with IC50 of 0.311 and 5.5 μM[1][2][3].

IC 50

PARP-1: 0.311 μM (IC₅₀); Aurora A: 5.5 μM (IC₅₀); hA₁AR: 4.6 μM (Ki); hA_2AAR: 4.8 μM (Ki)

References

[1] van der Horst E, et al., Multi-objective evolutionary design of adenosine receptor ligands. J Chem Inf Model. 2012 Jul 23;52(7):1713-21. DOI:10.1021/ci2005115
[2] Ferraris D, et al., Design and synthesis of poly ADP-ribose polymerase-1 inhibitors. 2. Biological evaluation of aza-5[H]-phenanthridin-6-ones as potent, aqueous-soluble compounds for the treatment of ischemic injuries. J Med Chem. 2003 Jul 3;46(14):3138-51. DOI:10.1021/jm030109s
[3] Karra S, et al., SAR and evaluation of novel 5H-benzo[c][1,8]naphthyridin-6-one analogs as Aurora kinase inhibitors. Bioorg Med Chem Lett. 2013 May 15;23(10):3081-7. DOI:10.1016/j.bmcl.2013.03.008