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Background: On the basis that various substituted salicylamides have shown interesting biological properties, we designed and synthesized new salicylamide derivatives with dipeptide moieties. Methods: The synthesis was based on the gradual building of target molecules and provided optically pure compounds. Conclusion: The obtained compounds were tested for their antiproliferative effect against three leukaemia cell lines in vitro and displayed GI50 values in the mid-micromolar range.