Wilkening R R, Ratcliffe R W, Fried A K, Meng D, Sun W, Colwell L, Lambert S, Greenlee M, Nilsson S, Thorsell A, Mojena M, Tudela C, Frisch K, Chan W, Birzin E T, Rohrer S P, Hammond M L
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, 800-B116 Rahway, NJ 07065, USA.
Bioorg Med Chem Lett. 2006 Aug 1;16(15):3896-901. doi: 10.1016/j.bmcl.2006.05.036. Epub 2006 May 30.
Synthesis of a series of fused pyrazole tetrahydrofluorenone analogs which are potent, ERbeta subtype selective ligands is described. Analogs possessing subnanomolar ERbeta binding, greater than 100-fold ERbeta-selectivity, and oral bioavailability are reported.
本文描述了一系列具有强效、雌激素受体β（ERβ）亚型选择性的稠合吡唑四氢芴酮类似物的合成。报道了具有亚纳摩尔ERβ结合力、大于100倍的ERβ选择性和口服生物利用度的类似物。
