Synthesis, Cytostatic, Antimicrobial, and Anti-HCV Activity of 6-Substituted 7-(Het)aryl-7-deazapurine Ribonucleosides
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- 作者：Petr Nau? ; Olga Caletková ; Petr Kone?ny ; Petr D?ubák ; Kate?ina Bogdanová ; Milan Kolá? ; Jana Vrbková ; Lenka Slavětínská ; Eva Tlou?t’ová ; Pavla Perlíková ; Marián Hajdúch ; Michal Hocek
- 刊名：Journal of Medicinal Chemistry
- 出版年：2014
- 出版时间：February 13, 2014
- 年：2014
- 卷：57
- 期：3
- 页码：1097-1110
- 全文大小：508K
- ISSN：1520-4804
文摘
A series of 80 7-(het)aryl- and 7-ethynyl-7-deazapurine ribonucleosides bearing a methoxy, methylsulfanyl, methylamino, dimethylamino, methyl, or oxo group at position 6, or 2,6-disubstituted derivatives bearing a methyl or amino group at position 2, were prepared, and the biological activity of the compounds was studied and compared with that of the parent 7-(het)aryl-7-deazaadenosine series. Several of the compounds, in particular 6-substituted 7-deazapurine derivatives bearing a furyl or ethynyl group at position 7, were significantly cytotoxic at low nanomolar concentrations whereas most were much less potent or inactive. Promising activity was observed with some compounds against Mycobacterium bovis and also against hepatitis C virus in a replicon assay.