2. Academic Validation
  3. 2-(3-Amino-3-deoxy-beta-D-xylofuranosyl)thiazole-4-carboxamide: a new tiazofurin analogue with potent antitumour activity

2-(3-Amino-3-deoxy-beta-D-xylofuranosyl)thiazole-4-carboxamide: a new tiazofurin analogue with potent antitumour activity

  • Bioorg Med Chem Lett. 2006 Oct 15;16(20):5317-20. doi: 10.1016/j.bmcl.2006.07.086.
Mirjana Popsavin 1,  Sasa Spaić,  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. mpopsavin@ih.ns.ac.yu
PMID: 16908146 DOI: 10.1016/j.bmcl.2006.07.086
Abstract

A new tiazofurin analogue, 2-(3-amino-3-deoxy-beta-d-xylofuranosyl)thiazole-4-carboxamide (3), was synthesized starting from d-glucose and evaluated for its in vitro antiproliferative activity against a panel of human tumour cell lines. Compound 3 exhibited the most powerful cytotoxicity against K562 cells, being approximately 100-fold more potent than tiazofurin. This analogue was also active against Jurkat, HT-29 and HeLa malignant cells, with respective IC(50) values being CA. 2-, 27- and 17-fold lower than those observed for tiazofurin. Remarkably, compound 3 did not exhibit any significant cytotoxicity towards normal foetal lung MRC-5 cell line.

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