Table 3. Inhibition of P. falciparum Growth and pfHDAC-1 Activity by Cherry-Picked Hits from the HDAC-Biased Chemical Library.

compd	R	n	pfHDAC-1, IC50 (nM)	fold change in MM.1S histone acetylationa	P. falciparum3D7, IC50 (nM)
8	3-hydroxyphenyl	5	59 ± 6	1.2	99 ± 12
9	2,5-dihydroxyphenyl	6	110 ± 13	1.1	142 ± 28
10	6-bromobenzo[d][1,3]dioxol-5-yl	5	20 ± 2	1.0	59 ± 15
11	2,4,6-trishydroxyphenyl	6	43 ± 5	1.1	50 ± 6
12	2-bromo-5-methoxyphenyl	5	22 ± 2	1.1	>500
13	4-(dimethylamino)-2-hydroxyphenyl	5	37 ± 4	1.2	24 ± 2
14	2-hydroxynaphthalen-1-yl	5	41 ± 4	1.0	20 ± 2
15	2-bromo-5-hydroxyphenyl	5	49 ± 5	1.0	35 ± 4
16	2-bromophenyl	5	37 ± 4	1.1	15 ± 2
17	2-bromo-4-hydroxy-5-methoxyphenyl	5	59 ± 7	1.0	47 ± 7
18	2-chlorophenyl	5	90 ± 10	0.9	288 ± 20
19	4-(1H-imidazol-1-yl)phenyl	5	15 ± 2	1.0	57 ± 11
20	2-bromopyridin-3-yl	5	36 ± 6	0.9	22 ± 5
21	2-bromo-4-hydroxyphenyl	4	106 ± 11	1.1	53 ± 13
22	2-bromo-5-hydroxyphenyl	4	89 ± 9	1.1	30 ± 7
23	2-bromo-4-hydroxy-5-methoxyphenyl	4	59 ± 5	1.2	498 ± 168
24	4-boronophenyl	4	45 ± 5	1.0	68 ± 8

^aThe fold change in MM.1S histone acetylation was measured at a compound concentration of 0.2 μM.