Table 2. Further SAR Explorations.
extraction ratios |
||||||
---|---|---|---|---|---|---|
R1 | R2 | IGF-1R cell mechanistica IC50 (μM) | IR cell mechanisticb IC50 (μM) | mouse | human | |
9a | H | 0.15 | 0.70 | 0.62 | 0.71 | |
9b | F | 0.017 | 0.076 | 0.43 | 0.55 | |
11a | H | CHO | 0.026 | 0.26 | 0.24 | 0.66 |
11b | F | CHO | 0.008 | 0.048 | 0.44 | 0.65 |
11c | H | CH3 | 0.025 | 0.32 | 0.52 | 0.64 |
11d | F | CH3 | 0.014 | 0.068 | 0.44 | 0.50 |
LISN cell line.
HepG2 cell line.