Synthesis and enzymatic evaluation of pyridinium-substituted uracil derivatives as novel inhibitors of thymidine phosphorylase
Synthesis and enzymatic evaluation of pyridinium-substituted uracil derivatives as novel inhibitors of thymidine phosphorylase
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DOI：
10.1016/s0968-0896(01)00309-1
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发表时间：
2002-03-01
影响因子：
3.5
通讯作者：
Freeman, S
中科院分区：
文献类型：
--
作者：
Murray, PE;McNally, VA;Freeman, S
制备了一系列水溶性N(1)-和C(6)-取代的尿嘧啶吡啶鎓化合物作为胸苷磷酸化酶(TP)的潜在抑制剂。 C(6)-尿嘧啶取代的衍生物是最活跃的。 1-[(5-氯-2,4-二羟基-嘧啶-6-基)甲基]氯化吡啶被确定为最好的抑制剂，其效力比已知抑制剂 6-氨基-5-溴尿嘧啶强 5 倍。 (C) 2002 Elsevier Science Ltd. 保留所有权利。
A series of water soluble N(1)- and C(6)-substituted uracil pyridinium compounds were prepared as potential inhibitors of thymidine phosphorylase (TP). The C(6)-uracil substituted derivatives were the most active. 1-[(5-Chloro-2,4-dihydroxy-pyrimidin-6-yl)methyl]pyridinium chloride, was identified as the best inhibitor being 5-fold more potent than the known inhibitor, 6-amino-5-bromouracil. (C) 2002 Elsevier Science Ltd. All rights reserved.