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. Author manuscript; available in PMC: 2024 May 20.
Published in final edited form as: J Med Chem. 2024 Mar 29;67(7):5333–5350. doi: 10.1021/acs.jmedchem.3c01596

Table 1.

SAR study of substitutions on the pyridine and benzimidazoline imine

graphic file with name nihms-1990869-t0011.jpg
No. R1 R2 R3 IC50 (nM)a

SI-2 H H H 22
6a F H H 5.4
6b F F H 2.5
6c (SI-12) F F F 3.4
6d H F F 6.3
6e F Cl Cl 18
6f COOCH3 F F 2.9
6g CONH2 F F 2.7
6h graphic file with name nihms-1990869-t0012.jpg F F 6.7
6i graphic file with name nihms-1990869-t0013.jpg F F 30.5
6j graphic file with name nihms-1990869-t0014.jpg F F 44.7
6k graphic file with name nihms-1990869-t0015.jpg F F 249
6l COOH F F >1000
6m graphic file with name nihms-1990869-t0016.jpg F F >1000
a

The cytotoxicity activities of individual compound to MCF7 cells were determined by the MTT assay. Data are the mean of triplicate determinations.