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. Author manuscript; available in PMC: 2018 Aug 1.
Published in final edited form as: Bioorg Med Chem. 2017 May 19;25(15):3947–3963. doi: 10.1016/j.bmc.2017.05.032

Table 4.

SAR of the indoles that were designed, synthesized, and tested.

graphic file with name nihms883163u4.jpg
Cmpd X Y G R1 R2 R3 R4 IC50 (μM) LE
16 N NH2 Et H H H H 29.2 0.32
17 CH Me Me H H H H 124 0.30
18 CH Me Et H H H H 10.2 0.36
19 CH Me Me H Me H H 8.53 0.36
20 CH Me Et H Me H H 3.37 0.37
21 CH Me Et H Me F H 4.52 0.35
22 CH Me Et H Me H F 8.26 0.33
23 CH Me Et H Me F F 7.76 0.32
24 CH Me Et CH2OMe Me H H 3.9 0.32
25 CH Me Me (CH2)2OMe Me H H 1.33 0.35
26 CH Me Et (CH2)2OMe Me H H 0.23 0.38
27 CH Me Et (CH2)2OMe Me F H 0.06 0.39
28 CH Me Et (CH2)2OMe Me H F 0.36 0.35
29 CH Me Et (CH2)2OMe Me F F 0.11 0.36
30 CH Me Et (CH2)3OMe Me H H 0.22 0.36
31 CH Me Et (CH2)2CONHMe Me H H 1.93 0.29