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ANALOGS OF BENZAMIDE, FOR USE AS PARP (ADP-RIBOSYL TRANSFERASE, ADPRT) DNA REPAIR CYCLE INHIBITORS
ANALOGS OF BENZAMIDE, FOR USE AS PARP (ADP-RIBOSYL TRANSFERASE, ADPRT) DNA REPAIR CYCLE INHIBITORS
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机译：苯甲酰胺的类似物，用作PARP（ADP-核糖基转移酶，ADPRT）DNA修复周期抑制剂
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摘要
A range of benzamide analogues consisting of 3-oxybenzamide derivatives are disclosed which can act as potent inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase or PARP enzyme (EC 2.4.2.30), and which thereby can provide useful therapeutic compounds for use in conjunction with DNA-damaging cytotoxic drugs or radiotherapy to potentiate the effects of the latter. The compounds disclosed include certain benzoxazole-4-carboxamide compounds and in general they comprise compounds having the general structural formula I CHEM or pharmaceutically acceptable salt thereof, characterised in that Y and X together form a bridge -Y-X- that represents the grouping CHEM where R5 is H, alkyl or an optionally substituted aralkyl or aryl group.
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