Journal
FUTURE MEDICINAL CHEMISTRY
Volume 13, Issue 13, Pages 1127-+Publisher
FUTURE SCI LTD
DOI: 10.4155/fmc-2020-0379
Keywords
antitumor; cancer; peptoid; solid-phase synthesis
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Funding
- CONICET (PUE-2016)
- ANPCyT [PICT 2017-2694, PICT 2017-1278]
- Agencia Santafesina de Ciencia, Tecnica e Innovacion (ASACTEI) [AC - 2015-00005]
- Universidad Nacional de Rosario [BIO 514]
- CONICET [PIP 0154]
- Universidad de Buenos Aires [UBACYT 20020170100041BA]
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This study synthesized and evaluated a library of peptoid analogs, with peptoid 4e showing the highest antiproliferative activity among the tested compounds, indicating its potential as a promising antitumor drug candidate.
Aim: 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 the reference compound, TAP7f, was investigated. In addition, the effect of the triazole linking group on the biological activity of these new derivatives was evaluated, exchanging it with a glycine spacer. The cytotoxic 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. [GRAPHICS] .
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