Tentoxin as a Scaffold for Drug Discovery. Total Solid-Phase Synthesis of Tentoxin and a Library of Analogues

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 genera...

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Veröffentlicht in:Organic letters 2003-06, Vol.5 (12), p.2115-2118
Hauptverfasser: Jiménez, Jose C, Chavarría, Bibiana, López-Macià, Àngel, Royo, Miriam, Giralt, Ernest, Albericio, Fernando
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container_end_page 2118
container_issue 12
container_start_page 2115
container_title Organic letters
container_volume 5
creator Jiménez, Jose C
Chavarría, Bibiana
López-Macià, Àngel
Royo, Miriam
Giralt, Ernest
Albericio, Fernando
description 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.
doi_str_mv 10.1021/ol0345273
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subjects Amino Acid Sequence
Combinatorial Chemistry Techniques
Mycotoxins - analogs & derivatives
Mycotoxins - chemical synthesis
Peptides, Cyclic - chemical synthesis
Peptides, Cyclic - chemistry
Structure-Activity Relationship
title Tentoxin as a Scaffold for Drug Discovery. Total Solid-Phase Synthesis of Tentoxin and a Library of Analogues
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