Title of article :
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)
Author/Authors :
Martin Stockley، نويسنده , , William Clegg، نويسنده , , Gabriele Fontana، نويسنده , , Bernard T. Golding، نويسنده , , Niall Martin، نويسنده , , Laurent J. M. Rigoreau، نويسنده , , Graeme C. M. Smith، نويسنده , , Roger J. Griffin، نويسنده ,
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 IC50 value of 100 μM was determined for inhibition of DNA-PK, and this is approximately 12-fold higher than that reported previously.
