Synthesis, crystal structure determination, and biological properties of the DNA-dependent protein kinase (DNA-PK) inhibitor 3-cyano-6-hydrazonomethyl-5-(4-pyridyl)pyrid-[1H]-2-one (OK-1035)

  • Bioorg Med Chem Lett. 2001 Nov 5;11(21):2837-41. doi: 10.1016/s0960-894x(01)00537-6.
M Stockley  1 ,  W Clegg ,  G Fontana ,  B T Golding ,  N Martin ,  L J Rigoreau ,  G C Smith ,  R J Griffin
Affiliations
  • 1. Department of Chemistry, Bedson Building, The University, Newcastle upon Tyne NE1 7RU, UK.
PMID: 11597411 DOI: 10.1016/s0960-894x(01)00537-6
Abstract

The first reported synthesis of the DNA-PK Inhibitor 3-cyano-6-hydrazonomethyl-5-(4-pyridyl)pyrid-[1H]-2-one (OK-1035) is described. The structure of OK-1035 was validated by X-ray crystallography. An IC(50) value of 100 microM was determined for inhibition of DNA-PK, and this is approximately 12-fold higher than that reported previously.

Products