Table 1. Substitution at the 4-Position of Aniline SARa.
IC50 (nM) |
|||
---|---|---|---|
compd | R | ACHN | HT-29 |
4a | H | 10000 (1) | 1300 (1) |
4b | Me | 1300 (2) | 110 (2) |
4c | Et | 185 (3) | 27 (3) |
4d | Pr | 2100 (2) | 230 (2) |
4e | cPr | 290 (2) | 39 (2) |
4f | vinyl | 104 (3) | 15 (3) |
4g | C≡CH (ethynyl) | 42 (2) | 5.9 (2) |
4h | C≡C−Me | >3000 (1) | >1000 (1) |
4i | CN | >10000 (1) | 1600 (1) |
4j | F | >3000 (1) | >1000 (1) |
4k | Cl | 4600 (2) | 102 (2) |
4l | Br | 325 (4) | 15 (4) |
4m | I | 13 (2) | 1.5 (2) |
Numbers in parentheses represent numbers of determinations.