Tentoxin as a scaffold for drug discovery. Total s...[Org Lett. 2003]

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1: Org Lett. 2003 Jun 12;5(12):2115-8. Links

Tentoxin as a scaffold for drug discovery. Total solid-phase synthesis of tentoxin and a library of analogues.

Jiménez JC, Chavarría B, López-Macià A, Royo M, Giralt E, Albericio F.

Barcelona Biomedical Research Institute and Combinatorial Chemistry Unity, Barcelona Science Park, University of Barcelona, Josep Samitier 1, 08028-Barcelona, Spain.

[reaction: see text] A solid-phase method for the synthesis of tentoxin has been developed. Two key steps-dehydration and N-alkylation-are carried out while the peptide is anchored to the resin. The method, which has been validated by the preparation of a library of tentoxin analogues, should be applicable to the generation of further libraries that have the tentoxin scaffold structure, as well as other structures containing N-alkylated didehydroamino acids.

PMID: 12790542 [PubMed - indexed for MEDLINE]

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[Curr Protein Pept Sci. 2008]
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