Synthesis and biological activity of novel N6-substituted and 2,N6-disubstituted adenine ribo- and 3'-C-methyl-ribonucleosides as antitumor agents.


:A series of N6-aminopurine-9-β-D-ribonucleosides and ribose-modified 3'-C-methyl analogues substituted at N6-position with a small group like hydroxy, methoxy or amino group or at C2(N6) position have been synthesized and tested against a panel of human leukemia and carcinoma cell lines. N6-Hydrazino-9-β-D-ribofuranosyl-purine (5) displayed the best antiproliferative activity in the low micromolar or submicromolar range against all tested tumor cell lines. The activity of this nucleoside is related in part to ribonucleotide reductase inhibition. C2-modification or 3'-C-methylation in N6-substituted adenosine analogues leads to a decrease or loss in activity.


Eur J Med Chem


Cappellacci L,Petrelli R,Franchetti P,Vita P,Kusumanchi P,Kumar M,Jayaram HN,Zhou B,Yen Y,Grifantini M




Has Abstract


2011-05-01 00:00:00














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    pub_type: 杂志文章,评审


    authors: Venepally V,Reddy Jala RC

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    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章


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    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章,评审


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    journal_title:European journal of medicinal chemistry

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    authors: Moloney GP,Garavelas A,Martin GR,Maxwell M,Glen RC

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    abstract::In this study synthesis and β-glucuronidase inhibitory potential of 3/5/8 sulfonamide and 8-sulfonate derivatives of quinoline (1-40) are discussed. Studies reveal that all the synthetic compounds were found to have good inhibitory activity against β-glucuronidase. Nonetheless, compounds 1, 2, 5, 13, and 22-24 having ...

    journal_title:European journal of medicinal chemistry

    pub_type: 杂志文章


    authors: Bano B,Arshia,Khan KM,Kanwal,Fatima B,Taha M,Ismail NH,Wadood A,Ghufran M,Perveen S

    更新日期:2017-10-20 00:00:00