Syntheses of N3-substituted thymine acyclic nucleoside phosphonates and a comparison of their inhibitory effect towards thymidine phosphorylase
Result description
A series of N3-substituted thymine acyclic nucleoside phosphonates bearing a number of (phosphonomethoxy)alkyl groups were synthesized and investigated for their ability to inhibit the human thymidine phosphorylase expressed in V79 Chinese hamster cells,as well as thymidine phosphorylase from SD-lymphoma, Escherichia coli and human placenta. In comparison to N1- substituted analogues which possess a considerable inhibitory activity towards thymidine phosphorylase from SD-lymphoma, the results showed amarginal inhibitory effect of these compounds. None of the presented N3-substituted derivatives possess a significant cytostatic activity.
Keywords
acyclic nucleoside phosphonatesthymidine phosphorylasefluorinationpyrimidine
The result's identifiers
Result code in IS VaVaI
Result on the web
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DOI - Digital Object Identifier
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Alternative languages
Result language
angličtina
Original language name
Syntheses of N3-substituted thymine acyclic nucleoside phosphonates and a comparison of their inhibitory effect towards thymidine phosphorylase
Original language description
A series of N3-substituted thymine acyclic nucleoside phosphonates bearing a number of (phosphonomethoxy)alkyl groups were synthesized and investigated for their ability to inhibit the human thymidine phosphorylase expressed in V79 Chinese hamster cells,as well as thymidine phosphorylase from SD-lymphoma, Escherichia coli and human placenta. In comparison to N1- substituted analogues which possess a considerable inhibitory activity towards thymidine phosphorylase from SD-lymphoma, the results showed amarginal inhibitory effect of these compounds. None of the presented N3-substituted derivatives possess a significant cytostatic activity.
Czech name
Syntézy N3-substituovaných thyminových acyklických nukleosidových fosfonátů a zhodnocení jejich inhibičního účinku vůči thymidinfosforylase
Czech description
Řada N3-substituovaných acyklických nukleosidových fosfonátů nesoucích (fosfonomethoxy)alkylové skupiny byly připraveny a testovány pro jejich schopnost inhibovat lidskou thymidinfosforylasu exprimovanou z V79 buňek činských křečků stejně jako vůči thymidinfosforylasám z SD-lymfomu, Escherichia coli a lidské placenty. V porovnání z N1-substituovanými analogy, které mají významnou inhibiční aktivitu vůči thymidinfosforylase z SD-lymfomu, výsledky ukázaly nedostatečný inhibiční efekt těchto sloučenin. Žádný z prezentovaných N3-substituovaných derivátů nemá významnou cytostatickou aktivitu.
Classification
Type
Jx - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)
CEP classification
CC - Organic chemistry
OECD FORD branch
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Result continuities
Project
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Continuities
Z - Vyzkumny zamer (s odkazem do CEZ)
Others
Publication year
2008
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
Bioorganic and Medicinal Chemistry Letters
ISSN
0960-894X
e-ISSN
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Volume of the periodical
18
Issue of the periodical within the volume
4
Country of publishing house
GB - UNITED KINGDOM
Number of pages
4
Pages from-to
1364-1367
UT code for WoS article
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EID of the result in the Scopus database
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Result type
Jx - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)
CEP
CC - Organic chemistry
Year of implementation
2008