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. Author manuscript; available in PMC: 2010 Aug 13.
Published in final edited form as: J Med Chem. 2009 Aug 13;52(15):4604–4612. doi: 10.1021/jm9002999

Table 2.

IC50 values of Sdex and Oxdex Py-Im polyamide conjugates from in vitro GR competition binding assays.

Compound IC50 (nM) Compound IC50 (nM)
ImPy7γ̃βDa-Sdex (6) 14 ± 0.87 ImPy7γ-Et-Sdex (16) 27 ± 2.1
ImPy6γ̃βDa-Sdex (7) 20 ± 1.1 ImPy6γ-Et-Sdex (17) 21 ± 1.7
ImPy5γ̃βDa-Sdex (8) 22 ± 2.9 ImPy5γ-Et-Sdex (18) 21 ± 2.3
ImPy4γ̃βDa-Sdex (9) 16 ± 1.1 ImPy4γ-Et-Sdex (19) 23 ± 2.6
ImPy4-βDa-Sdex (10) 16 ± 2.0 ImPy4-Et-Sdex (20) 34 ± 2.5
ImPy3-βDa-Sdex (11) 20 ± 1.1 ImPy3-Et-Sdex (21) 26 ± 1.8
ImPy2-βDa-Sdex (12) 12 ± 0.82 ImPy2-Et-Sdex (22) 14 ± 0.80
ImPy-βDa-Sdex (13) 8.5 ±0.43 ImPy-Et-Sdex (23) 5.7 ± 0.30

ImPy7γ-Et-Oxdex (24) 840 ± 130 Ac-Et-Sdex (15) 9.8 ± 0.88
ImPy3-Et-Oxdex (25) 550 ± 57 Ac-Da-Sdex (28) 8.3 ± 0.61
Impy2-Et-Oxdex (26) 480 ± 69 Ac-βDa-Sdex (14) 9.3 ± 0.48
ImPy-Et-Oxdex (27) 460 ± 42 dexamethasonea (1) 5 ± 1
Oxdex-CONH2 c (4) 600 ± 100 IBA-Sdexb (5) 15 ± 1.5
a, c

Reference 15.

b

Reference 20.