Background: Structural component of proteins and peptides, amino acids have been
used as building blocks in the synthesis of more complex molecules with antitumor activity against
several types of cancer.
Objective: The search for new anticancer compounds is ongoing, especially for cancers that are
very aggressive and have poor prognoses, such as leukemia.
Method: Here, we report a method to synthesize Tyr-Tyr dipeptides via sonochemistry reactions followed
by functionalization of these Tyr-Tyr dipeptides with Suzuki-Miyaura and Sonogashira crosscoupling
reactions in good yields. Twelve different Tyr-Tyr dipeptides were investigated against
three cell lines: HaCaT; Jurkat-E6; and A2058.
Results: Some of the Tyr-Tyr dipeptides showed activity against Jurkat-E6 leukaemia cells at low
concentration, decreasing their viability, but not against non-tumor HaCaT cells, suggesting a
cytotoxicity specific to tumor cells.
Conclusion: All dipeptides were able to decrease the viability of Jurkat cell line, however the
A2058 cell line did not respond well to treatment with the peptides. Some of the modified Tyr-Tyr
dipeptides presented selective activity on leukemic tumor cells.