Nucleoside phosphonic acids in thymidine phosphorylase inhibition: structure-activity relationship.
A number of structurally diverse nucleoside phosphonic acids have been tested against human recombinant thymidine phosphorylase and human platelets supernatant using 2'-deoxy-5-nitrouridine as the substrate. We have selected several inhibitors working at micromolar level as lead structures for further evaluation.
Panova
Natalya
N
Institute of Organic Chemistry and Biochemistry, Czech Academy of Sciences, Flemingovo n. 2, 166 10 Prague 6, Czech Republic.
Kosiová
Ivana
I
Petrová
Magdalena
M
Vanĕk
Václav
V
Liboska
Radek
R
Kovacková
Sona
S
Kocalka
Petr
P
Králíková
Sárka
S
Tocík
Zdenĕk
Z
Páv
Ondrej
O
Paces
Ondrej
O
Rejman
Dominik
D
Rosenberg
Ivan
I
D000818:Animals; D001792:Blood Platelets / Q000201:enzymology; D016466:CHO Cells; D006224:Cricetinae; D003412:Cricetulus; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D009705:Nucleosides / Q000737:chemistry* / Q000494:pharmacology*; D063065:Organophosphonates / Q000737:chemistry*; D013329:Structure-Activity Relationship; D013939:Thymidine Phosphorylase / Q000037:antagonists & inhibitors* / Q000737:chemistry
D004791:Enzyme Inhibitors; D009705:Nucleosides; D063065:Organophosphonates; D013939:Thymidine Phosphorylase