Synthesis and evaluation of substituted chroman-4-one and chromone derivatives as sirtuin 2-selective inhibitors

…, T Suuronen, M Lahtela-Kakkonen…

文献索引：Huhtiniemi, Tero; Suuronen, Tiina; Rinne, Valtteri M.; Wittekindt, Carsten; Lahtela-Kakkonen, Maija; Jarho, Elina; Wallen, Erik A. A.; Salminen, Antero; Poso, Antti; Leppaenen, Jukka Journal of Medicinal Chemistry, 2008 , vol. 51, # 15 p. 4377 - 4380

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被引用次数: 41

摘要

A series of substituted chromone/chroman-4-one derivatives has been synthesized and evaluated as novel inhibitors of SIRT2, an enzyme involved in aging-related diseases, eg, neurodegenerative disorders. The analogues were efficiently synthesized in a one-step procedure including a base-mediated aldol condensation using microwave irradiation. The most potent compounds, with inhibitory concentrations in the low micromolar range, were ...