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.
