Table 1.
SAR study of substitutions on the pyridine and benzimidazoline imine
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---|---|---|---|---|
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 |
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F | F | 6.7 |
6i |
![]() |
F | F | 30.5 |
6j |
![]() |
F | F | 44.7 |
6k |
![]() |
F | F | 249 |
6l | COOH | F | F | >1000 |
6m |
![]() |
F | F | >1000 |
The cytotoxicity activities of individual compound to MCF7 cells were determined by the MTT assay. Data are the mean of triplicate determinations.