A series of N(3)-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 N(1)- substituted analogues which possess a considerable inhibitory activity towards thymidine phosphorylase from SD-lymphoma, the results showed a marginal inhibitory effect of these compounds. None of the presented N(3)-substituted derivatives possess a significant cytostatic activity.
- MeSH
- Cricetulus MeSH
- financování organizované MeSH
- inhibitory enzymů farmakologie chemická syntéza MeSH
- křečci praví MeSH
- krysa rodu rattus MeSH
- lidé MeSH
- lymfom T-buněčný enzymologie MeSH
- organofosfonáty farmakologie chemická syntéza MeSH
- placenta enzymologie MeSH
- pyrimidinové nukleosidy farmakologie chemická syntéza MeSH
- thymidinfosforylasa antagonisté a inhibitory MeSH
- thymin analogy a deriváty farmakologie chemická syntéza MeSH
- vztahy mezi strukturou a aktivitou MeSH
- zvířata MeSH
- Check Tag
- křečci praví MeSH
- krysa rodu rattus MeSH
- lidé MeSH
- zvířata MeSH
- MeSH
- financování organizované MeSH
- Publikační typ
- abstrakty MeSH