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…
Index: Stockley; Clegg; Fontana; Golding; Martin; Rigoreau; Smith; Griffin Bioorganic and medicinal chemistry letters, 2001 , vol. 11, # 21 p. 2837 - 2841
Full Text: HTML
Citation Number: 29
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.
Related Articles:
[White; Deerberg Chemical Communications, 1997 , # 19 p. 1919 - 1920]
[Organic and Biomolecular Chemistry, , vol. 10, # 17 p. 3472 - 3485]
Hydroxyacyl derivatives of forskolin—their positive inotropic activity
[Bioorganic and Medicinal Chemistry, , vol. 6, # 11 p. 2061 - 2073]