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N-(3-(4-Hydroxyphenyl)-propenoyl)-amino acid tryptamides as SIRT2 inhibitors
Authors:Kiviranta Päivi H  Leppänen Jukka  Rinne Valtteri M  Suuronen Tiina  Kyrylenko Olga  Kyrylenko Sergiy  Kuusisto Erkki  Tervo Anu J  Järvinen Tomi  Salminen Antero  Poso Antti  Wallén Erik A A
Affiliation:Department of Pharmaceutical Chemistry, University of Kuopio, PO Box 1627, 70211 Kuopio, Finland. paivi.kiviranta@uku.fi
Abstract:A series of N-(3-(4-hydroxyphenyl)-propenoyl)-amino acid tryptamides was based on a previously reported new SIRT2 inhibitor from our group, and it was designed to study if the molecular size of the compound could be reduced. The most potent compounds, N-(3-(4-hydroxyphenyl)-propenoyl)-2-aminoisobutyric acid tryptamide and N-(3-(4-hydroxyphenyl)-propenoyl)-L-alanine tryptamide, were equipotent, 30% smaller in molecular weight, and slightly more selective (SIRT2/SIRT1) than the parent compound.
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