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Chroman-4-one and chromone based somatostatin beta-turn mimetics

Journal article
Authors Maria Fridén-Saxin
Tina Seifert
Marcus Malo
Krystle da Silva Andersson
Nils Pemberton
Christine Dyrager
Annika Friberg
Kristian Dahlén
Erik A A Wallén
Morten Grøtli
Kristina Luthman
Published in European Journal of Medicinal Chemistry
Volume 114
Pages 59-64
ISSN 0223-5234
Publication year 2016
Published at Department of Chemistry and Molecular Biology
Pages 59-64
Language en
Keywords Chromone, Chroman-4-one, Peptidomimetics, Somatostatin, binding affinities, nonpeptide peptidomimetics, natural-products, analog, receptors, scaffolds, design, conformation, polypeptide, peptides, Pharmacology & Pharmacy
Subject categories Pharmacology


A scaffold approach has been used to develop somatostatin beta-turn mimetics based on chroman-4-one and chromone ring systems. Such derivatives could adopt conformations resembling type II or type II' beta-turns. Side chain equivalents of the crucial Trp8 and Lys9 in somatostatin were introduced in the 2- and 8-positions of the scaffolds using efficient reactions. Interestingly, this proof-of-concept study shows that 4 and 9 have K-i-values in the low mu M range when evaluated for their affinity for the sst2 and sst4 receptors. (C) 2016 Elsevier Masson SAS. All rights reserved.

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