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. 2021 Dec 29;23(1):369. doi: 10.3390/ijms23010369

Table 1.

Inhibitory activity of the synthesized compounds against class I HDACs.

graphic file with name ijms-23-00369-i001.jpg

Cpd. No. X Y R 1 R 2 R 3 HDAC1
(IC50 µM)		 HDAC2
(IC50 µM)		 HDAC3
(IC50 µM)		 HDAC8
(% Inhib.)
19a CH N graphic file with name ijms-23-00369-i002.jpg H H 0.51 ± 0.05 0.80 ± 0.07 1.12 ± 0.07 0% @ 1 µM
19b CH N graphic file with name ijms-23-00369-i003.jpg H H 25.8% @ 2 µM 30.3% @ 2 µM 65.2% @2 µM 3.4% @ 1 µM
19c N CH graphic file with name ijms-23-00369-i004.jpg H H 33.9% @ 2 µM 20.1% @ 2 µM 26.8% @2 µM 0% @ 1 µM
19d CH N graphic file with name ijms-23-00369-i005.jpg H H 0.52 ± 0.07 1.43 ± 0.08 1.06 ± 0.04 0% @ 1 µM
19e CH N graphic file with name ijms-23-00369-i006.jpg H H 0.21 ± 0.07 0.71 ± 0.04 0.84 ± 0.03 0% @ 1 µM
19f CH N graphic file with name ijms-23-00369-i007.jpg H H 0.13 ± 0.01 0.28 ± 0.01 0.31 ± 0.01 0% @ 1 µM
19g CH N graphic file with name ijms-23-00369-i008.jpg H H 0.31 ± 0.03 0.96 ± 0.05 0.49 ± 0.06 0% @ 1 µM
19h CH N graphic file with name ijms-23-00369-i009.jpg F F 0.81 ± 0.07 0.74 ± 0.03 0.57 ± 0.02 n.d.
19i CH N graphic file with name ijms-23-00369-i010.jpg Cl H 3.0 ± 0.2 2.7 ± 0.2 1.9 ± 0.1 n.d.
19j N CH graphic file with name ijms-23-00369-i011.jpg H H 0.45 ± 0.06 0.93 ± 0.04 1.75 ± 0.06 0% @ 1 µM
19k CH N graphic file with name ijms-23-00369-i012.jpg H H 0.14 ± 0.02 0.56 ± 0.04 0.59 ± 0.03 0% @ 1 µM
19l CH N graphic file with name ijms-23-00369-i013.jpg F F 0.29 ± 0.03 0.56 ± 0.02 0.81 ± 0.05 n.d.
19m CH N graphic file with name ijms-23-00369-i014.jpg F H 0.40 ± 0.06 1.48 ± 0.19 0.40 ± 0.02 n.d.
19n N CH CH3 H H 5% @ 1 µM 7% @ 1 µM 13% @ 1 µM n.d.
19o CH N CH3 H H 27% @ 1 µM 15% @ 1 µM 30% @ 1 µM n.d.
21a CH N graphic file with name ijms-23-00369-i015.jpg H 2-Thienyl 0.26 ± 0.01 2.47 ± 0.22 0% @ 1 µM n.d.
21b CH N graphic file with name ijms-23-00369-i016.jpg H 4-F-C6H4 0.70 ± 0.08 0.77 ± 0.06 0% @ 1 µM 0% @ 1 µM
21c CH N graphic file with name ijms-23-00369-i017.jpg H 2-F-C6H4 0.76 ± 0.07 0.76 ± 0.04 15 ± 1 0% @ 1 µM
23a CH N H F H 3.30 ± 0.18 2.20 ± 0.20 0.40 ± 0.01 0% @ 1 µM
23b CH N graphic file with name ijms-23-00369-i018.jpg H F 0.27 ± 0.03 0.50 ± 0.03 0.50 ± 0.02 38% @ 1 µM
23c CH N graphic file with name ijms-23-00369-i019.jpg H F 0.33 ± 0.02 1.37 ± 0.08 0.59 ± 0.04 n.d.
25a CH N H Cl H 0% @ 1 µM 0% @ 1 µM 8.7 ± 0.4 n.d.
25b CH N H F F 4.3 ± 0.3 4.2 ± 0.10 1.6 ± 0.1 n.d.
27a CH N H H CF3 0% @ 1 µM 0% @ 1 µM 0% @ 1 µM n.d.
27b CH N H CH3 H 0% @ 1 µM 0% @ 1 µM 0% @ 1 µM n.d.
27c CH N H OCH3 H 20.0 ± 1.0 14.0 ± 2.0 14.0 ± 1.0 n.d.
29a CH N CH3 H 3-Thienyl 0.11 ± 0.01 0.18 ± 0.06 4.4 ± 0.1 n.d.
29b CH N H H 2-Thienyl 0.07 ± 0.01 0.26 ± 0.01 6.1 ± 0.7 n.d.
29c CH N H H 4-F-C6H4 0.16 ± 0.03 0.34 ± 0.01 6.7 ± 0.5 n.d.
29d CH N CH3 H 2-F-C6H4 0.18 ± 0.01 0.26 ± 0.07 12.0 ± 1.0 n.d.
CI994 -- -- -- -- -- 37% @ 1 µM 36% @ 1 µM 32% @ 1 µM n.d.
RGFP-966 -- -- -- -- -- 16 ± 2 11 ± 1 1.3 ± 0.1 n.d.
MS-275 -- -- -- -- -- 0.93 ± 0.1 0.95 ± 0.03 1.8 ± 0.1 n.d.
Mocetinostat -- -- -- -- -- 0.33 ± 0.04 0.34 ± 0.01 0.93 ± 0.05 n.d.

n.d. not determined, -- no substituents.