Synthesis, crystal structure determination, and biological properties of the DNA-dependent protein kinase (DNA-PK) inhibitor 3-cyano-6-hydrazonomethyl-5-(4-pyridyl) …

M Stockley, W Clegg, G Fontana, BT Golding…

文献索引：Stockley; Clegg; Fontana; Golding; Martin; Rigoreau; Smith; Griffin Bioorganic and medicinal chemistry letters, 2001 , vol. 11, # 21 p. 2837 - 2841

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被引用次数: 29

摘要

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.