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. Author manuscript; available in PMC: 2024 Nov 12.
Published in final edited form as: J Med Chem. 2023 Jan 26;66(3):1928–1940. doi: 10.1021/acs.jmedchem.2c01731

Table 3.

SAR of the indole ring of anthranilic acid series using a Topliss tree-like exploration of all the available synthetic sites

graphic file with name nihms-2031880-t0015.jpg
Compound X R2 R4 R5 R6 R7 IC50
(p-Cl-ANS, μM)
TW-8-67-2 NH H H H H H 4.6
24 NMe H H H H H 21
25 O H H H H H 32
26 NH Me H H H H 16
27 NH H Me H H H 5.0
28 NH H Cl H H H 3.9
29 NH H H Me H H 21
30 NH H H Cl H H 5.8
31 NH H H H H Me 24
32 NH H H H H Cl 15
33 NH H H H Me H 0.92
34 NH H H H Cl H 0.44
35 NH H H H F H 0.37
36 NH H H H Br H 0.25