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Issue 8, 2013
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Synthesis and biological evaluation of a post-synthetically modified Trp-based diketopiperazine

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Abstract

A series of C2-arylated analogues of the diketopiperazine brevianamide F has been synthesized using a mild Pd-catalyzed CH-activation procedure. Biological evaluation of the new derivatives in different cell lines shows that this modification is responsible for the remarkable change in activity, turning a mild antibiotic and antifungal natural product (brevianamide F) into novel antitumoral compounds. Furthermore, the approach stated represents a new straightforward and versatile methodology with promising applications in peptidomimetics and medicinal chemistry.

Graphical abstract: Synthesis and biological evaluation of a post-synthetically modified Trp-based diketopiperazine

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Publication details

The article was received on 23 Nov 2012, accepted on 07 Jun 2013 and first published on 10 Jun 2013


Article type: Concise Article
DOI: 10.1039/C3MD20353K
Med. Chem. Commun., 2013,4, 1171-1174

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    Synthesis and biological evaluation of a post-synthetically modified Trp-based diketopiperazine

    S. Preciado, L. Mendive-Tapia, C. Torres-García, R. Zamudio-Vázquez, V. Soto-Cerrato, R. Pérez-Tomás, F. Albericio, E. Nicolás and R. Lavilla, Med. Chem. Commun., 2013, 4, 1171
    DOI: 10.1039/C3MD20353K

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