Chroman-4-one and chromone based somatostatin β-turn mimetics.

Fridén-Saxin M, Seifert T, Malo M, da Silva Andersson K, Pemberton N, Dyrager C, Friberg A, Dahlén K, Wallén EA, Grøtli M, Luthman K

Eur J Med Chem 114 (-) 59-64 [2016-05-23; online 2016-02-21]

A scaffold approach has been used to develop somatostatin β-turn mimetics based on chroman-4-one and chromone ring systems. Such derivatives could adopt conformations resembling type II or type II' β-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 Ki-values in the low μM range when evaluated for their affinity for the sst2 and sst4 receptors.

Swedish NMR Centre (SNC) [Service]

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PubMed 26974375

DOI 10.1016/j.ejmech.2016.02.046

Crossref 10.1016/j.ejmech.2016.02.046

S0223-5234(16)30136-2