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

Encouraged by the antitumor activity exhibited by triazolylpeptidyl penicillins, we decided to synthesize and evaluate a library of peptoid analogs. The replacement of the dipeptide unit of the reference compound, TAP7f, was investigated. In addition, the effect of the triazole linking group on the...

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Published inFuture medicinal chemistry Vol. 13; no. 13; pp. 1127 - 1139
Main Authors Martiren, Nadia L, Bellizzi, Yanina, Barrionuevo, Elizabeth, Blank, Viviana C, Roguin, Leonor P, Mata, Ernesto G, Cornier, Patricia G
Format Journal Article
LanguageEnglish
Published England Newlands Press Ltd 01.07.2021
Subjects
antitumor
cancer
peptoid
solid-phase synthesis
cancer
antitumor
peptoid
solid-phase synthesis
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Summary:Encouraged by the antitumor activity exhibited by triazolylpeptidyl penicillins, we decided to synthesize and evaluate a library of peptoid analogs. 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. Among the tested compounds, peptoid exhibited the highest antiproliferative activity.
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ISSN:1756-8919
1756-8927
DOI:10.4155/fmc-2020-0379