6-SUBSTITUTED 5-FLUOROURACIL DERIVATIVES AS TRANSITION STATE ANALOGUE INHIBITORS OF THYMIDINE PHOSPHORYLASE

@article{Kalman20056SUBSTITUTED5D,
  title={6-SUBSTITUTED 5-FLUOROURACIL DERIVATIVES AS TRANSITION STATE ANALOGUE INHIBITORS OF THYMIDINE PHOSPHORYLASE},
  author={T. Kalman and Li Lai},
  journal={Nucleosides, Nucleotides \& Nucleic Acids},
  year={2005},
  volume={24},
  pages={367 - 373}
}
  • T. Kalman, Li Lai
  • Published 2005
  • Chemistry, Medicine
  • Nucleosides, Nucleotides & Nucleic Acids
A combination of mechanism-based and structure-based design strategies led to the synthesis of a series of 5- and 6-substituted uracil derivatives as potential inhibitors of thymidine phosphorlase/platelet derived endothelial cell growth factor (TP/PD-ECGF). Among those tested, 6-imidazolylmethyl-5-fluorouracil was found to be the most potent inhibitor with a Ki-value of 51 nM, representing a new class of 5-fluoropyrimidines with a novel mechanism of action. 
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Evolution of uracil based thymidine phosphorylase inhibitors, SAR and electronic correlation: revisit
Synthesis and in Vitro Evaluation of 5-Fluoro-6-[(2-Iminopyrrolidin-1-YL)Methyl]Uracil, TPI(F): An Inhibitor of Human Thymidine Phosphorylase (TP)
Efficient one-pot synthesis of polysubstituted 6-[(1 H -1,2,3-triazol-1-yl)methyl]uracils through the “click” protocol
Electroreductive coupling of 1,3-dimethyluracils with aromatic ketones: synthesis of 6-substituted 1,3-dimethyluracils
Preparation method of tipiracil intermediate
Structural investigation of the thymidine phosphorylase from Salmonella typhimurium in the unliganded state and its complexes with thymidine and uridine.
Electroreductive Intermolecular Coupling of Uracils with Aromatic Ketones: Synthesis of 6-Substituted and cis-5,6-Disubstituted 5,6-Dihydro-1,3-dimethyluracils and Their Transformation to 6-Substituted 1,3-Dimethyluracils, trans-5,6-Disubstituted 5,6-Dihydro-1,3-dimethyluracils, and 4,5,5-Trisubstit
Stereoselective capture of N-acyliminium ions generated from α-hydroxy-N-acylcarbamides: direct synthesis of uracils from barbituric acids enabled by SmI2 reduction.
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