. Author manuscript; available in PMC: 2019 Jun 1.

Published in final edited form as: Org Lett. 2018 May 23;20(11):3255–3258. doi: 10.1021/acs.orglett.8b01118

Table 1.

Activities of 4a–m, vorinostat, HPOB and Tubastatin A against HDAC1 and HDAC6.

entry	R¹	R²	HDAC1 IC₅₀ [μM]	HDAC6 IC₅₀ [μM]	SF^a
4a		H	0.13(±0.014)	0.050(±0.00035)	3
4b		H	0.89(±0.012)	0.074(±0.0063)	12
4c		H	0.51(±0.057)	0.051(±0.0033)	10
4d		H	0.66(±0.033)	0.12(±0.036)	6
4e		H	0.18(±0.018)	0.14(±0.024)	<2
4f		H	0.17(±0.029)	0.064(±0.0047)	3
4g		H	>3.333	1.33(±0.22)	>3
4h		H	0.27(±0.019)	0.10(±0.0041)	3
4i	H	H	0.84(±0.062)	0.076(±0.0036)	11
4j	H	7-Me	1.01(±0.0035)	0.069(±0.0039)	15
4k	H	6-Me	0.75(±0.043)	0.071(±0.0054)	11
4l		H	2.20(±0.33)	0.058(±0.012)	38
4m		H	1.31(±0.086)	0.057(±0.0034)	23

		vorinostat	0.10(±0.0058)	0.030(±0.0040)	3
		HPOB	2.10(±0.23)	0.085(±0.0090)	25
		Tubastatin A	2.49(±0.14)	0.014(±0.00061)	178

Selectivity factor (SF = IC₅₀ (HDAC1)/IC₅₀ (HDAC6)).