Table 1. Results from Evaluation of Compounds 1a–p, 3a,b, and 4–6 in a SIRT2 Activity Assay.

compd	R2	R6	R7	R8	inhibition ± SD at 200 μM (%)a	IC50 (μM)b,c
1a	(CH2)4CH3	Cl	H	Br	88 ± 0.9	4.3 (3.5–5.4)
(+)-1a	(CH2)4CH3	Cl	H	Br	70 ± 0.8	4.5 (3.5–5.9)
(−)-1a	(CH2)4CH3	Cl	H	Br	91 ± 0.8	1.5 (1.3–1.7)
1b	(CH2)4CH3	H	H	H	4.9 ± 4.8	n.d.
1c	(CH2)4CH3	Br	H	Br	92 ± 1.2	1.5 (1.3–1.7)
1d	(CH2)4CH3	CH3	H	CH3	83 ± 0.7	6.2 (4.7–8.1)
1e	(CH2)4CH3	F	H	F	30 ± 1.3	n.d.
1f	(CH2)4CH3	Cl	H	H	55 ± 2.4	n.d.
1g	(CH2)4CH3	NO2	H	H	58 ± 0.7	n.d.
1h	(CH2)4CH3	OCH3	H	H	20 ± 4.1	n.d.
1i	(CH2)4CH3	H	H	Br	28 ± 1.1	n.d.
1j	(CH2)4CH3	H	F	H	18 ± 1.0	n.d.
1k	(CH2)2CH3	Cl	H	Br	76 ± 1.8	10.6 (9.0–12.5)
1l	(CH2)6CH3	Cl	H	Br	57 ± 2.5	n.d.
1m	CH2CH2Ph	Cl	H	Br	81 ± 0.7	6.8 (5.8–8.0)
1n	CH(CH3)2	Cl	H	Br	52 ± 1.0	n.d.
1o	CH2CH2(3-indolyl)	Cl	H	Br	53 ± 1.7	n.d.
1p	CH2CH2(N-Ts)(3-indolyl)	Cl	H	Br	27 ± 1.6	n.d.
3a	(CH2)4CH3	Cl	H	Br	82 ± 0.4	5.5 (4.8–6.2)
3b	Ph	Cl	H	Br	20 ± 1.4	n.d.
4	(CH2)4CH3	Cl	H	Br	31 ± 3.0	n.d.
5	(CH2)4CH3	Cl	H	Br	38 ± 1.3	n.d.
6	(CH2)4CH3	Cl	H	Br	38 ± 1.2	n.d.

^aSD, standard deviation (n = 3).

^bIC₅₀ (95% confidence interval). IC₅₀ values were determined for compounds showing >70% inhibition of SIRT2 at 200 μM concentration.

^cn.d. = not determined