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Title: Preparation of penta-azole containing cyclopeptides: challenges in macrocyclization
Author: Hernández Romero, Delia
Riego, Estela
Francesch, Andrés
Cuevas, Carmen
Albericio Palomera, Fernando
Álvarez Domingo, Mercedes
Keywords: Productes naturals
Síntesi orgànica
Compostos heterocíclics
Natural products
Organic synthesis
Heterocyclic compounds
Issue Date: 10-Jul-2007
Publisher: Elsevier B.V.
Abstract: Herein is described the synthesis of several analogs of the natural product IB-01211 from concatenated azoles, via a biomimetic pathway based on cyclization-oxidation of serine containing peptides combined with the Hantzsch synthesis. The macrocyclization of rigid peptide compounds 1 and 2 to give IB-01211 and its epimer 12b was explored, and the results are compared here to those previously obtained for the macrocyclization of more flexible structures in the syntheses of YM-216391, telomestatin, and IB-01211. Lastly, the preliminary results of anti-tumor activity screening of the synthesized analogs are discussed.
Note: Versió postprint del document publicat a:
It is part of: Tetrahedron, 2007, vol. 63, num. 39, p. 9862-9870
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ISSN: 0040-4020
Appears in Collections:Articles publicats en revistes (Farmacologia, Toxicologia i Química Terapèutica)

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