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Structural diversity of nucleoside phosphonic acids as a key factor in the discovery of potent inhibitors of rat T-cell lymphoma thymidine phosphorylase

SYSNO ASEP	0345860
Document Type	J - Journal Article
R&D Document Type	Journal Article
Subsidiary J	Článek ve WOS
Title	Structural diversity of nucleoside phosphonic acids as a key factor in the discovery of potent inhibitors of rat T-cell lymphoma thymidine phosphorylase
Author(s)	Kočalka, Petr (UOCHB-X) Rejman, Dominik (UOCHB-X)_{RID, ORCID} Vaněk, Václav (UOCHB-X)_{RID, ORCID} Rinnová, Markéta (UOCHB-X) Tomečková, Ivana (UOCHB-X) Králíková, Šárka (UOCHB-X)_RID Petrová, Magdalena (UOCHB-X)_RID Páv, Ondřej (UOCHB-X)_{RID, ORCID} Pohl, Radek (UOCHB-X)_{RID, ORCID} Buděšínský, Miloš (UOCHB-X)_{RID, ORCID} Liboska, Radek (UOCHB-X)_{RID, ORCID} Točík, Zdeněk (UOCHB-X) Panova, Natalya (UOCHB-X)_RID Votruba, Ivan (UOCHB-X)_RID Rosenberg, Ivan (UOCHB-X)_{RID, ORCID}
Number of authors	15
Source Title	Bioorganic and Medicinal Chemistry Letters. - : Elsevier - ISSN 0960-894X Roč. 20, č. 3 (2010), s. 862-865
Number of pages	4 s.
Language	eng - English
Country	GB - United Kingdom
Keywords	phosphonate nucleotides ; pyrrolidine ; thymidine phosphorylase
Subject RIV	CC - Organic Chemistry
R&D Projects	GA203/09/0820 GA ČR - Czech Science Foundation (CSF)
	GA202/09/0193 GA ČR - Czech Science Foundation (CSF)
	LC06061 GA MŠMT - Ministry of Education, Youth and Sports (MEYS)
	LC06077 GA MŠMT - Ministry of Education, Youth and Sports (MEYS)
	2B06065 GA MŠMT - Ministry of Education, Youth and Sports (MEYS)
	KAN200520801 GA AV ČR - Academy of Sciences of the Czech Republic (AV ČR)
	1QS400550501 GA AV ČR - Academy of Sciences of the Czech Republic (AV ČR)
	NR9138 GA MZd - Ministry of Health (MZ)
CEZ	AV0Z40550506 - UOCHB-X (2005-2011)
UT WOS	000273783800014
DOI	10.1016/j.bmcl.2009.12.081
Annotation	Structurally diverse, sugar-modified, thymine-containing nucleoside phosphonic acids were evaluated for their ability to inhibit thymidine phosphorylase purified from spontaneous T-cell lymphomas of an inbred Sprague-Dawley rat strain. From a large set of tested compounds, among them a number of pyrrolidine-based derivatives, 10 nucleotide analogues with IC50 values below 1 .mu.M were selected. Out of them, four compounds strongly inhibited the enzyme with IC50 values in a range of 11–45 nM. These most potent compounds might be bi-substrate analogues.
Workplace	Institute of Organic Chemistry and Biochemistry
Contact	asep@uochb.cas.cz ; Kateřina Šperková, Tel.: 232 002 584 ; Viktorie Chládková, Tel.: 232 002 434
Year of Publishing	2011

Number of the records: 1