6-Alkyl-, 6-aryl- or 6-hetaryl-7-deazapurine ribonucleosides as inhibitors of human or MTB adenosine kinase and potential antimycobacterial agents

0399777 - ÚOCHB 2014 RIV GB eng J - Journal Article
Perlíková, Pavla - Konečný, P. - Nauš, Petr - Snášel, Jan - Votruba, Ivan - Džubák, P. - Pichová, Iva - Hajdúch, M. - Hocek, Michal
6-Alkyl-, 6-aryl- or 6-hetaryl-7-deazapurine ribonucleosides as inhibitors of human or MTB adenosine kinase and potential antimycobacterial agents.
MedChemComm. Roč. 4, č. 11 (2013), s. 1497-1500. ISSN 2040-2503. E-ISSN 2040-2511
R&D Projects: GA ČR GAP207/11/0344
EU Projects: European Commission(XE) 241587 - SYSTEMTB
Grant - others:Operational Programme Research and Development for Innovations(XE) CZ.1.05/2.1.00/01.0030
Institutional support: RVO:61388963
Keywords : mycobacterium-tuberculosis * enzyme-inhibition * 6-(het)aryl-7-deazapurine ribonucleosides
Subject RIV: CC - Organic Chemistry
Impact factor: 2.626, year: 2013

Title 6-alkyl-, 6-aryl- and 6-hetaryl-7-deazapurine ribonucleosides previously known as nanomolar cytostatics were found to be potent inhibitors of either human or mycobacterial (MTB) adenosine kinase (ADK). Several new derivatives bearing bulky substituents at position 6 were non-cytotoxic but selectively inhibited MTB ADK. However, most of the nucleosides (ADK inhibitors) as well as their octadecylphosphate prodrugs were inactive in the whole cell assay of inhibition of Mycobacterium bovis growth. 6-Methyl-7-deazapurine ribonucleoside was found to be a potent antimycobacterial agent.
Permanent Link: http://hdl.handle.net/11104/0227143