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PDBsum entry 2iog
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References listed in PDB file
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Key reference
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Title
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Estrogen receptor ligands. Part 16: 2-Aryl indoles as highly subtype selective ligands for eralpha.
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Authors
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K.D.Dykstra,
L.Guo,
E.T.Birzin,
W.Chan,
Y.T.Yang,
E.C.Hayes,
C.A.Dasilva,
L.Y.Pai,
R.T.Mosley,
B.Kraker,
P.M.Fitzgerald,
F.Dininno,
S.P.Rohrer,
J.M.Schaeffer,
M.L.Hammond.
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Ref.
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Bioorg Med Chem Lett, 2007,
17,
2322-2328.
[DOI no: ]
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PubMed id
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Abstract
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A novel class of indole ligands for estrogen receptor alpha have been discovered
which exhibit potent affinity and high selectivity. Substitution of the
bazedoxifene skeleton to the linker present in the HTS lead 1a provided 22b
which was found to be 130-fold alpha-selective and acted as an antagonist of
estradiol activity in uterine tissue and MCF-7 cancer cells.
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