共 11 条
[11]
SHARMA AP, 1990, J MED CHEM, V33, P3229
Estrogen receptor ligands.: Part 4:: The SAR of the syn-dihydrobenzoxathiin SERAMs
被引：34
作者：
Kim, S
Wu, J
Chen, HY
Birzin, ET
Chan, WD
Yang, YT
Colwell, L
Li, S
Dahllund, J
DiNinno, F
Rohrer, SP
Schaeffer, JM
Hammond, ML
机构：
[1] Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA
[2] Merck Res Labs, Dept Atherosclerosis & Endocrinol, Rahway, NJ 07065 USA
[3] Kar Biol AB, Novum, S-14157 Huddinge, Sweden
关键词：
SERM;
benzoxathiin;
estrogen;
D O I：
10.1016/j.bmcl.2004.03.074
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of estrogen receptor ligands based on a dihydrobenzoxathiin scaffold is described and evaluated for estrogen/anti-estrogen activity in both in vitro and in vivo models. The most active analogue, 22, was found to be 40-fold ERalpha selective in a competitive binding assay, and 22 demonstrated very potent in vivo antagonism of estradiol driven proliferation in an immature rat uterine weight gain assay. (C) 2004 Elsevier Ltd. All rights reserved.
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页码：2741 / 2745
页数：5
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