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. Author manuscript; available in PMC: 2022 Sep 26.

Published in final edited form as: Bioorg Med Chem Lett. 2020 Sep 12;30(24):127543. doi: 10.1016/j.bmcl.2020.127543

Table 1.

CpIMPDH and HsIMPDH inhibitory activities of 8 – 17.


Compound	R¹	R²	R³	CpIMPDH K_i,app (μM)	HsIMPDH K_i,app (μM)
8	3-OMe, 4-Cl	H	H	0.046 (±0.013)^σ	0.35 (±0.09)^σ
9	3,4-di-Cl	H	H	0.041 (±0.010)^σ	0.34 (± 0.11)^σ
10	3-CF₃, 4-Cl	H	H	0.016 (±0.007)^σ	0.23 (±0.08)^σ
11	2,3-di-Cl	H	H	0.681 (0.143)^r	ND^*
12	4-Cl	H	H	0.042 (±0.02)^σ	0.13 (±0.05)^σ
13	4-F	H	H	0.180 (±0.06)^r	0.27
14	4-CF₃	H	H	0.151 (±0.04)^r	0.40
15	4-CN	H	H	0.11	0.35
16	4-Cl	Me	H	0.87 (±0.13)^r	ND^*
17	3-CF₃ 4-Cl	H	Me	1.7	ND^*

^*

ND: Not Determined

^σ:

Standard deviation

^r:

Range