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. Author manuscript; available in PMC: 2022 Dec 15.
Published in final edited form as: Bioorg Med Chem Lett. 2021 Nov 9;54:128443. doi: 10.1016/j.bmcl.2021.128443

Table 1.

SAR among representative class A’ analogs (1 – 19)

graphic file with name nihms-1758270-t0002.jpg
Compound A B C IC50 ± SE (nM)
1 4-FPh Ph Me 25 ± 2
2 4-FPh 4-(MeO)Ph Me 1,360 ± 150
3 4-FPh 3-(MeO)Ph Me 108 ± 6
4 4-FPh 2-(MeO)Ph Me 75 ± 7.4
5 4-FPh t-Bu Me 153 ± 14
6 4-ClPh Ph Me 252 ± 21
7 2,4-Cl2Ph Ph Me >100,000
8 t-Bu 2-Pyr Me 850 ± 140
9 4-FPh Ph MeO(CH2)2 123 ± 8.7
10 Ph Ph PhCH2 100 ± 14
11 4-Pyr Ph Me 541 ± 21
12 4-FPh 3-Pyr Me 213 ± 24
13 4-FPh 4-Pyr Me 17,400 ± 1300
14 4-FPh 2-Pyr Me 14 ± 1.1
15 4-FPh 3-Me-2-Pyr Me 8.7 ± 0.74
16 4-FPh 2-Pyr Allyl 5.5 ± 0.39
17 4-FPh 3-Me-2-Pyr graphic file with name nihms-1758270-t0003.jpg 43 ± 2.4
18 4-FPh 3-Me-2-Pyr 3-PyrCH2 36 ± 3.1
19 4-NH2Ph 3-Me-2-Pyr Me 29 ± 2.7