| 摘要 |
The instant application describes novel compounds that modulate (in particular, inhibit) Sirt2, with structures according to Formulas (1) and (2) provided herein. The invention is also directed to pharmaceutical compositions thereof, methods of treatment (i.e., cancer and neurodegenerative disease) by administration of the modulating compounds, assay methods for finding modulators of Sirt2, and kits for practicing the assay method. |
| 主权项 |
1. A compound that modulates Sirt2 activity having the following chemical structure: wherein R1 is a hydrocarbon group having at least five carbon atoms connected by carbon-carbon bonds, wherein said hydrocarbon group optionally includes one heteroatom group selected from —O—, —NR5—, and —S— that interrupts a carbon-carbon bond of said hydrocarbon group, and wherein one or more hydrogen atoms in said hydrocarbon group are optionally replaced with fluoro atoms, wherein R5 is a hydrogen atom or a hydrocarbon group; R2 is selected from a hydrogen atom or a hydrocarbon group; R6 and R7 are independently selected from hydrogen atom, unsubstituted hydrocarbon groups having up to six carbon atoms, alkoxy groups —OR, amide groups —NR′C(O)R or —C(O)NR′R, ketone groups —C(O)R, ester groups —C(O)OR or —OC(O)R, carbamate groups —OC(O)NR′R or —NR′C(O)OR, and urea groups —NR′C(O)NR, wherein R is a hydrocarbon group having up to six carbon atoms, and R′ is a hydrogen atom or a hydrocarbon group having up to six carbon atoms; X1, X2, and X3 are independently selected from —(CH2)n—, —NR—, —O—, —S—, or a bond, wherein n represents 1, 2, or 3, and at least one of X1, X2, and X3 is a —CH2 group; and Y1 and Y2 are independently selected from —O—, —NR5—, and —S— groups. |
