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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.

graphic file with name nihms295016u2.jpg
compd Substituents R1, R2, R3 IC50 ± SD (nM) HDAC8/HDAC3a
HDAC3 HDAC8
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 graphic file with name nihms295016t2.jpg 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)