2. Academic Validation
  3. Synthesis and antiproliferative activity of two new tiazofurin analogues with 2'-amido functionalities

Synthesis and antiproliferative activity of two new tiazofurin analogues with 2'-amido functionalities

  • Bioorg Med Chem Lett. 2006 May 15;16(10):2773-6. doi: 10.1016/j.bmcl.2006.02.001.
Mirjana Popsavin 1,  Ljilja Torović,  Milos Svircev,  Vesna Kojić,  Gordana Bogdanović,  Velimir Popsavin
Affiliations

Affiliation

  • 1 Department of Chemistry, Faculty of Sciences, University of Novi Sad, Trg D. Obradovića 3, 21000 Novi Sad, Serbia and Montenegro. mpopsavin@ih.ns.ac.yu
PMID: 16495053 DOI: 10.1016/j.bmcl.2006.02.001
Abstract

Two novel tiazofurin analogues 2 and 3 were synthesized starting from d-glucose. The key step of the synthesis was the efficient one-step hydrogen sulfide-mediated conversion of 2-azido-3-O-acyl-ribofuranosyl cyanides to the corresponding 2-amido thiocarboxamides. Compounds 2 and 3 were evaluated for their in vitro antiproliferative activity against certain human tumour cell lines. Remarkably, compound 2 was found to be 570-fold more potent than tiazofurin against MCF-7 cells, while compound 3 showed the most powerful cytotoxicity against HT-29 Cancer cells, being almost 100-fold more active than tiazofurin.

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