Design, synthesis and cytotoxic evaluation of peptoid analogs of an anticancer active triazolylpeptidyl penicillin

NADIA L MARTIREN; YANINA BELLIZZI; ELIZABETH BARRIONUEVO; VIVIANA C BLANK; LEONOR P. ROGUIN; ERNESTO G. MATA; PATRICIA G. CORNIER

Future Medicinal Chemistry

Newlands Press

Año: 2021 vol. 13 p. 1127 - 1139

1756-8919

Encouraged by the antitumor activity exhibited by triazolylpeptidyl penicillins, we decided to synthesize and evaluate a library of peptoid analogs. Results: The replacement of the dipeptide unit of thereference compound, TAP7f, was investigated. In addition, the effect of the triazole linking group onthe biological activity of these new derivatives was evaluated, exchanging it with a glycine spacer. Thecytotoxic effect of the library compounds was determined in the B16-F0 cell line and compared with the effects on normal murine mammary gland cells. Conclusion: Among the tested compounds, peptoid 4e exhibited the highest antiproliferative activity