869006-52-0Relevant articles and documents
ANTIESTROGEN COMPOUNDS
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, (2020/01/08)
A genus of proteolysis-targeting chimeras (PROTACs)-type compounds/antiestrogens has now been found that act as selective estrogen receptor degraders (SERDs) and estrogen receptor antagonists by degrading and antagonizing ERa in breast cancer cells. The compounds are of the following genus: The compounds described herein exhibit anti-proliferative effects, and are potentially useful, alone or in combination with other therapies, for the treatment of breast cancer. In general, these compounds combine a tight binding ERa targeting ligand tethered to a recognition motif or degron. Once bound, the degron recruits destructive cellular components and the targeted receptor (i.e., ERa) is degraded (i.e., destroyed) or antagonized.
Estrogen receptor ligands. Part 14: Application of novel antagonist side chains to existing platforms
Blizzard, Timothy A.,Morgan II, Jerry D.,Chan, Wanda,Birzin, Elizabeth T.,Pai, Lee-Yuh,Hayes, Edward C.,DaSilva, Carolyn A.,Mosley, Ralph T.,Yang, Yi Tien,Rohrer, Susan P.,Dininno, Frank,Hammond, Milton L.
, p. 5124 - 5128 (2007/10/03)
Two novel side chains which had previously been found to enhance antagonist activity in the dihydrobenzoxathiin SERM series were applied to three existing platforms. The novel side chains did not improve the antagonist activity of the existing platforms.
