N-(3-(4-Hydroxyphenyl)-propenoyl)-amino acid tryptamides as SIRT2 inhibitors |
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| 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 |
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| Affiliation: | Department of Pharmaceutical Chemistry, University of Kuopio, PO Box 1627, 70211 Kuopio, Finland. paivi.kiviranta@uku.fi |
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| 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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