Synthesis and enzymatic evaluation of xanthine oxidase-activated prodrugs based on inhibitors of thymidine phosphorylase

…, E Chinje, IJ Stratford, KT Douglas, S Freeman

Index: Reigan, Philip; Gbaj, Abdul; Chinje, Edwin; Stratford, Ian J.; Douglas, Kenneth T.; Freeman, Sally Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 21 p. 5247 - 5250

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Citation Number: 20

Abstract

A series of xanthine oxidase-activated prodrugs of known inhibitors of thymidine phosphorylase has been designed and synthesised to introduce tumour selectivity. These prodrugs were oxidised by xanthine oxidase at C-2 and/or C-4 of the uracil ring to generate the desired TP inhibitor.