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EJNMMI Radiopharmacy and Chemistry

Table 1 Potency of 1–6 in a T47D alkaline phosphatase assays, including Tanaproget (TNP) as a reference compound

From: Synthesis of a benzoxazinthione derivative of tanaproget and pharmacological evaluation for PET imaging of PR expression

compd

cLogPc

T47D alkaline phosphatase assay EC50 (nM)a

T47D alkaline phosphatase assay IC50 (nM)a

TNP

4.16

0.5

–

1

2.98

> 10,000b

844.8 ± 0.23

2

4.17

4.7 ± 0.07

–

3

2.98

> 10,000b

795.0 ± 0.25

4

4.17

3674.0 ± 0.08

–

5

5.02

2294.0 ± 0.29

–

6

6.18

432.5 ± 0.24

–

  1. aExperimental values for 1–6 are presented as an average of at least n = 3 measurements ± standard deviation (SD).b The EC50 of 1 and 3 showed no agonist activity so IC50 values were calculated from the inhibition of progesterone (3 mM). c Calculated log P o/w from Chemdraw 12.0
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