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. Author manuscript; available in PMC: 2011 Aug 26.
Published in final edited form as: J Med Chem. 2010 Aug 26;53(16):6100–6111. doi: 10.1021/jm100507q

Table 1.

HDAC inhibition activity (IC50) and isoform selectivity of tricyclic ketolide-based HDAC inhibitors

Compd n Nuclear Extract (nM) HDAC 8 (nM) HDAC8:Nuclear Extract Isoform Selectivity HDAC 6 (nM) HDAC6:Nuclear Extract Isoform Selectivity
15a 1 7.77 796.2 102.5 1180.1 151.9
15b 2 1.03 544.6 528.7 728.7 707.5
15c 3 104.2 1909.3 18.3 1709.8 16.4
15d 4 163.6 2859.9 17.5 1916.9 11.7
15e 5 208.2 4557.8 21.9 3203.1 15.4
SAHAa 65.0 1860.0 29 85.5 1.3
a

Cited from ref. 22