Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1374108 | Bioorganic & Medicinal Chemistry Letters | 2006 | 4 Pages |
A new tiazofurin analogue, 2-(3-amino-3-deoxy-β-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 IC50 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.
Graphical abstractA new tiazofurin analogue 3 was synthesized starting from d-glucose and evaluated for its in vitro antiproliferative activity against a panel of human tumour cell lines.Figure optionsDownload full-size imageDownload as PowerPoint slide