Estrogen receptor ligands. Part 13: Dihydrobenzoxathiin SERAMs with an optimized antagonist side chain

被引:31
作者
Blizzard, TA [1 ]
DiNinno, F [1 ]
Chen, HY [1 ]
Kim, S [1 ]
Wu, JY [1 ]
Chan, WD [1 ]
Birzin, ET [1 ]
Yang, YT [1 ]
Pal, LY [1 ]
Hayes, EC [1 ]
DaSilva, CA [1 ]
Rohrer, SP [1 ]
Schaeffer, JM [1 ]
Hammond, ML [1 ]
机构
[1] Merck Res Labs, Rahway, NJ 07065 USA
关键词
SERMs; SERAMs; estrogen;
D O I
10.1016/j.bmcl.2005.05.089
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
An optimized side chain for dihydrobenzoxathim SERAMs was discovered and attached to four dihydrobenzoxathim platforms. The novel SERAMs show exceptional estrogen antagonist activity in uterine tissue and an MCF-7 breast cancer cell assay. (c) 2005 Elsevier Ltd. All rights reserved.
引用
收藏
页码:3912 / 3916
页数:5
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