Synthesis and enzymatic evaluation of pyridinium-substituted uracil derivatives as novel inhibitors of thymidine phosphorylase

Paul E. Murray; Virginia A. McNally; Stacey D. Lockyer; Kaye J. Williams; Ian J. Stratford; Mohammed Jaffar; Sally Freeman

doi:10.1016/S0968-0896(01)00309-1

Synthesis and enzymatic evaluation of pyridinium-substituted uracil derivatives as novel inhibitors of thymidine phosphorylase

Paul E. Murray, Virginia A. McNally, Stacey D. Lockyer, Kaye J. Williams, Ian J. Stratford, Mohammed Jaffar, Sally Freeman

Research output: Contribution to journal › Article › peer-review

Abstract

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-dihydroxypyrimidin-6-yl)methyl]pyridinium chloride, was identified as the best inhibitor being 5-fold more potent than the known inhibitor, 6-amino-5-bromouracil. © 2002 Elsevier Science Ltd. All rights reserved.

Original language	English
Pages (from-to)	525-530
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry
Volume	10
Issue number	3
DOIs	https://doi.org/10.1016/S0968-0896(01)00309-1
Publication status	Published - 2002

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title = "Synthesis and enzymatic evaluation of pyridinium-substituted uracil derivatives as novel inhibitors of thymidine phosphorylase",

abstract = "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-dihydroxypyrimidin-6-yl)methyl]pyridinium chloride, was identified as the best inhibitor being 5-fold more potent than the known inhibitor, 6-amino-5-bromouracil. {\textcopyright} 2002 Elsevier Science Ltd. All rights reserved.",

author = "Murray, {Paul E.} and McNally, {Virginia A.} and Lockyer, {Stacey D.} and Williams, {Kaye J.} and Stratford, {Ian J.} and Mohammed Jaffar and Sally Freeman",

year = "2002",

doi = "10.1016/S0968-0896(01)00309-1",

language = "English",

volume = "10",

pages = "525--530",

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T1 - Synthesis and enzymatic evaluation of pyridinium-substituted uracil derivatives as novel inhibitors of thymidine phosphorylase

AU - Murray, Paul E.

AU - McNally, Virginia A.

AU - Lockyer, Stacey D.

AU - Williams, Kaye J.

AU - Stratford, Ian J.

AU - Jaffar, Mohammed

AU - Freeman, Sally

PY - 2002

Y1 - 2002

N2 - 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-dihydroxypyrimidin-6-yl)methyl]pyridinium chloride, was identified as the best inhibitor being 5-fold more potent than the known inhibitor, 6-amino-5-bromouracil. © 2002 Elsevier Science Ltd. All rights reserved.

AB - 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-dihydroxypyrimidin-6-yl)methyl]pyridinium chloride, was identified as the best inhibitor being 5-fold more potent than the known inhibitor, 6-amino-5-bromouracil. © 2002 Elsevier Science Ltd. All rights reserved.

U2 - 10.1016/S0968-0896(01)00309-1

DO - 10.1016/S0968-0896(01)00309-1

M3 - Article

SN - 0968-0896

VL - 10

SP - 525

EP - 530

JO - Bioorganic and Medicinal Chemistry

JF - Bioorganic and Medicinal Chemistry

IS - 3

ER -

Synthesis and enzymatic evaluation of pyridinium-substituted uracil derivatives as novel inhibitors of thymidine phosphorylase

Abstract

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