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. Author manuscript; available in PMC: 2021 Apr 6.
Published in final edited form as: J Med Chem. 2020 Feb 14;63(5):2489–2510. doi: 10.1021/acs.jmedchem.9b01442

Table 1.

SAR of substituents and linkers of the 2-, 5- substituted benzoic acid core

graphic file with name nihms-1583434-t0012.jpg
Compound R1 Mcl-1 Ki (μM) Bfl-1 Ki (μM)
1 graphic file with name nihms-1583434-t0013.jpg 1.5 ± 0.3 1.6 ± 0.2
2 H 47.8 ± 3.9 >100
3 graphic file with name nihms-1583434-t0014.jpg 2.6 ± 0.4 3.0 ± 0.4
4 graphic file with name nihms-1583434-t0015.jpg 13.1 ± 2.4 14.8 ± 2.7
5 graphic file with name nihms-1583434-t0016.jpg 32.8 ± 4.9 >70
6 graphic file with name nihms-1583434-t0017.jpg 4.7 ± 0.7 3.8 ± 1.1
7 graphic file with name nihms-1583434-t0018.jpg 70.4 ± 5.4 >70
8 graphic file with name nihms-1583434-t0019.jpg 19.0 ± 1.2 62.0 ± 1.8
9 graphic file with name nihms-1583434-t0020.jpg 6.1 ± 1.0 10.6 ± 1.2
graphic file with name nihms-1583434-t0021.jpg
Compound R2 Mcl-1 Ki (μM) Bfl-1 Ki (μM)
10 H 3.4 ± 0.4 3.7 ± 0.4
11 graphic file with name nihms-1583434-t0022.jpg 2.7 ± 0.6 4.6 ± 0.5