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Issue 11, 2013
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6-Alkyl-, 6-aryl- or 6-hetaryl-7-deazapurine ribonucleosides as inhibitors of human or MTB adenosine kinase and potential antimycobacterial agents

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Abstract

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.

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

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Publication details

The article was received on 21 Aug 2013, accepted on 16 Sep 2013 and first published on 17 Sep 2013


Article type: Concise Article
DOI: 10.1039/C3MD00232B
Citation: Med. Chem. Commun., 2013,4, 1497-1500
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    6-Alkyl-, 6-aryl- or 6-hetaryl-7-deazapurine ribonucleosides as inhibitors of human or MTB adenosine kinase and potential antimycobacterial agents

    P. Perlíková, P. Konečný, P. Nauš, J. Snášel, I. Votruba, P. Džubák, I. Pichová, M. Hajdúch and M. Hocek, Med. Chem. Commun., 2013, 4, 1497
    DOI: 10.1039/C3MD00232B

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