Skip to main content
. Author manuscript; available in PMC: 2008 Nov 1.
Published in final edited form as: J Med Chem. 2007 Oct 5;50(22):5269–5280. doi: 10.1021/jm070556y

Table 5.

Summary of electrophilic compounds 8a–f: Yield, IC50 values of the inhibition between coregulatory peptide SRC2-2 and TRα/TRβ, viability (LD50) of U2OS and ARO cells in the presence of compound, solubility in PBS buffer containing 5% DMSO, and permeability across an artificial membrane (PAMPA).

In vitro Potency Cytotoxicity Pharmacological Properties
Entry R = 4-hexylbenzene Compound Yielda (%) TRαb IC50 (μM) TRβb IC50 (μM) TRα: TRβ ratio AROc LD50 (μM) U2OSc LD50 (μM) Solubility (μM) Permeability (10−6 cm/s)
1 graphic file with name nihms62751t17.jpg 8a 63 68.9 35.1 2.0 8.0 17.1 60 621
2 graphic file with name nihms62751t18.jpg 8b 57 16.7 6.2 2.7 7.9 13.9 18 21
3 graphic file with name nihms62751t19.jpg 8c 84 47.7 23.1 2.1 12.2 8.3 103 1029
4 graphic file with name nihms62751t20.jpg 8d 41 >100 >100 - 2.4 69 95 974
5 graphic file with name nihms62751t21.jpg 8e 69 4.2 3.0 1.4 40.1 17 85 1190
6 graphic file with name nihms62751t22.jpg 8f 95 >100 >100 - 28.7 25.3 26 58
7 graphic file with name nihms62751t23.jpg 8g 74 33.2 19.1 1.7 >200 58 204 1117
a

Isolated yield;

b

values are means of two independent experiments done in quadruplicate; the general error limits are 10%;

c

values are means of two independent experiments done in triplicate; the general error limits are 10–15%. Actual error values for each measurement are omitted for clarity but are included in tables in the supplemental materials.