| 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 method for treating a subject suffering from cancer, the method comprising administering to said subject a modulator of Sirt2 in a pharmaceutically effective amount for treating said cancer, the modulator of Sirt2 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; R3 and R4 are independently selected from hydrogen atom and hydrocarbon groups R, wherein said hydrocarbon groups R are optionally substituted with one or more heteroatoms; and X1, X2, and X3 are independently selected from —(CH2)n—, —NR5—, —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. |
