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) |
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| Authors: | Stockley M Clegg W Fontana G Golding B T Martin N Rigoreau L J Smith G C Griffin R J |
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| Institution: | Department of Chemistry, Bedson Building, The University, Newcastle upon Tyne NE1 7RU, UK. |
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| 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. |
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