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. 2010 Aug 30;1(9):510–515. doi: 10.1021/ml100178g

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
a

LISN cell line.

b

HepG2 cell line.