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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 29, Number 6
BKCSDE 29(6)
June 20, 2008 

Synthesis and Evaluation of Estrogen Receptor β-Selective Ligands: Fluoroalkylated Indazole Estrogens
Byung Seok Moon, John A. Katzenellenbogen, Gi Jeong Cheon, Dae Yoon Chi, Kyo Chul Lee*, Gwang Il An*
Estrogen receptor β, Indazole estrogen analogues, PET
It is important to identify selective ligands for the estrogen receptor subtypes ERα or ERβ to evaluate them as pharmaceutical targets in breast cancer. To develop ERβ-selective ligands as PET imaging agents, a series of aryl indazole estrogen analogues substituted at the C3 position with fluoroethyl and fluoropropyl groups were synthesized and evaluated for their relative binding affinities and selectivities for ERα vs ERβ. The fluoroethylated indazole estrogen (FEIE, 1i) and fluoropropylated indazole estrogen (FPIE, 1h) showed 41- fold and 17-fold ERβ/ERα selectivity, respectively. However, their binding affinities to ERα and ERβ were very low.
1107 - 1114
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