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. 
14 Citations
Kinetics and mechanistic study of competitive inhibition of thymidine phosphorylase by 5-fluoruracil derivatives.
Structural investigation of the thymidine phosphorylase from Salmonella typhimurium in the unliganded state and its complexes with thymidine and uridine.
...
1
2
...

References

SHOWING 1-10 OF 21 REFERENCES
Novel nonsubstrate inhibitors of human thymidine phosphorylase, a potential target for tumor-dependent angiogenesis.
Inhibition of thymidine phosphorylase by 6-aminothymine and derivatives of 6-aminouracil.
Crystal structure of human thymidine phosphorylase in complex with a small molecule inhibitor.
7‐Deazaxanthine, a novel prototype inhibitor of thymidine phosphorylase
Design of novel N-(2,4-dioxo-1,2,3,4-tetrahydro-thieno[3,2-d]pyrimidin-7-yl)-guanidines as thymidine phosphorylase inhibitors, and flexible docking to a homology model.
...
1
2
3
...