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. Author manuscript; available in PMC: 2021 Jun 7.

Published in final edited form as: J Med Chem. 2011 Dec 22;55(1):515–527. doi: 10.1021/jm2014277

Table 1.

SAR of ASP analogs with -S-, -SO-, -SO₂-, and -O- linkers^a



X	Compound	R	EC₅₀ (μM)

S	1	4-Cl	1.93
	2	2.6-diCl	0.71
	3	3,5-diCl	0.17

SO	4	4-Cl	> 32
SO	5	4-Cl-2,5-diMe	2.88

SO₂	6	4-Cl	4.7
	7	3,5-diCl	1.41
	8	4-Cl-2,5-diMe	1.47

O	9	4-Cl	0.79
	10	4-Et	1.96
	11	3-Et	0.72
	12	3-t-Bu	0.87
	13	3,5-diCl	0.067
	14	3,5-diCF₃	0.58
	15	3,5-diF	1.07
	16	3,5-diBr	0.51
	17	3-Br	1.02
	18	3-Ph	2.84
	19	3,5-diPh	3.70

^a

Average Z’ factor value = 0.5