Syntheses of 1-[2-(Phosphonomethoxy)Alkyl]Thymine Monophosphates and an Evaluation of their Inhibitory Activity Toward Human Thymidine Phosphorylase

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61388963%3A_____%2F12%3A00376556" target="_blank" >RIV/61388963:_____/12:00376556 - isvavai.cz</a>
Result on the web
<a href="http://dx.doi.org/10.1080/15257770.2011.648361" target="_blank" >http://dx.doi.org/10.1080/15257770.2011.648361</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1080/15257770.2011.648361" target="_blank" >10.1080/15257770.2011.648361</a>

Result language
angličtina
Original language name
Syntheses of 1-[2-(Phosphonomethoxy)Alkyl]Thymine Monophosphates and an Evaluation of their Inhibitory Activity Toward Human Thymidine Phosphorylase
Original language description
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 wereperformed 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 mu M, K-i(P-i)= 2.13 +/- 0.29 mu M) and (R) 3-MeO-PMPTp 4d (K-i(dT) = 5.78 +/- 0.71 mu M, K-i(P-i)= 2.71 +/- 0.37 mu M).
Czech name
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Czech description
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Type
J<sub>x</sub> - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)
CEP classification
CC - Organic chemistry
OECD FORD branch
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Project
<a href="/en/project/1M0508" target="_blank" >1M0508: New Antivirals and Antineoplastics</a><br>
Continuities
Z - Vyzkumny zamer (s odkazem do CEZ)

Publication year
2012
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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