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. Author manuscript; available in PMC: 2012 Oct 8.

Published in final edited form as: J Med Chem. 2011 Jun 2;54(13):4350–4364. doi: 10.1021/jm2001025

Table 2.

HDAC3 and HDAC8 isoform inhibitory activity (IC₅₀, nM) of pyrazole-based compounds 3a–3f.


compd	Substituents R₁, R₂, R₃	IC50 ± SD (nM)		HDAC8/HDAC3^a
compd	Substituents R₁, R₂, R₃	HDAC3	HDAC8	HDAC8/HDAC3^a
3a	R₁, R₂, R₃ = H	44 ± 5.8	76 ± 5.0	1.7
3b	R₂ = NO₂, R₁, R₃ = H	59 ± 1.0	82 ± 9.0	1.4
3c	R₂ = N₃ R₁, R₃ = H	22 ± 1.3	28 ± 3.0	1.3
3d	R₂ = NHBoc R₁, R₃ = H	191 ± 18	147 ± 15	0.8
3e		432 ± 52	487 ± 80	1.1
3f	R₁ = CH₂N₃ R₂ = H R₃ = N₃	128 ± 9.8	17 ± 3.0	0.13

^a

ratio of IC₅₀ (nM)