Syntheses of 1-[2-(Phosphonomethoxy)Alkyl] thymine monophosphates and an evaluation of their inhibitory activity toward human thymidine phosphorylase
Language English Country United States Media print
Document type Comparative Study, Journal Article, Research Support, Non-U.S. Gov't
- MeSH
- Cricetulus MeSH
- Phosphates MeSH
- Phosphorylation MeSH
- Kinetics MeSH
- Cricetinae MeSH
- Humans MeSH
- Molecular Structure MeSH
- Organophosphonates chemical synthesis chemistry metabolism pharmacology MeSH
- Thymidine MeSH
- Thymidine Phosphorylase antagonists & inhibitors MeSH
- Thymine analogs & derivatives chemical synthesis chemistry metabolism pharmacology MeSH
- Animals MeSH
- Check Tag
- Cricetinae MeSH
- Humans MeSH
- Animals MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Comparative Study MeSH
- Names of Substances
- 1-(3-fluoro-2-(phosphonomethoxy)propyl)thymine MeSH Browser
- Phosphates MeSH
- Organophosphonates MeSH
- Thymidine MeSH
- Thymidine Phosphorylase MeSH
- Thymine MeSH
A series of new monophosphates of 1-[2-(phosphonomethoxy)alkyl]thymines, such as PMPTp(,) 3-MeO-PMPTp, HPMPTp, and FPMPTp, were synthesized and tested for their ability to inhibit human thymidine phosphorylase. Kinetic measurements of enzyme activity were performed using thymidine and inorganic phosphate as the substrates. The data show that some monophosphates provide a considerable increase of the multisubstrate inhibitory effect. The highest inhibitory potency was found with (R)-FPMPTp 4c (K (i) (dT) = 4.09 ± 0.47 μM, K (i)(P(i)) = 2.13 ± 0.29 μM) and (R) 3-MeO-PMPTp 4d (K (i) (dT) = 5.78 ± 0.71 μM, K (i)(P(i)) = 2.71 ± 0.37 μM).
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