225222-73-1Relevant articles and documents
Facile synthesis of 3-aryl benzofurans, 3-aryl benzothiophenes, 2-aryl indoles and their dimers
Umareddy, Pailla,Arava, Veera Reddy
, p. 2156 - 2167 (2019/07/04)
The preparation of 3-aryl benzofuran and benzothiophenes and their dimers at 2-position and, 2-aryl indoles and their 3-position dimers preparation is described.
MODULATORS OF ESTROGEN RECEPTOR PROTEOLYSIS AND ASSOCIATED METHODS OF USE
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Paragraph 00498; 00499, (2018/08/20)
The present disclosure relates to bifunctional compounds, which find utility as modulators of estrogen receptor (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a cereblon, Von Hippel-Lindau ligase-binding moiety, Inhibitors of Apotosis Proteins, or mouse double-minute homolog 2 ligand, which binds to the respective E3 ubiquitin ligase, and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.
BENZOTHIOPHENE-BASED SELECTIVE MIXED ESTROGEN RECEPTOR DOWNREGULATORS
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Page/Page column 127, (2018/05/24)
This invention is benzothiophene-based selective mixed estrogen receptor downregulators and their compositions and uses to treat estrogen-related disorders.
Benzothiophene selective estrogen receptor modulators with modulated oxidative activity and receptor affinity
Qin, Zhihui,Kastrati, Irida,Chandrasena, R. Esala P.,Liu, Hong,Yao, Ping,Petukhov, Pavel A.,Bolton, Judy L.,Thatcher, Gregory R. J.
, p. 2682 - 2692 (2008/02/07)
The regulation of estrogenic and antiestrogenic effects of selective estrogen receptor modulators (SERMs) is thought to underlie their clinical use. Most SERMs are polyaromatic phenols susceptible to oxidative metabolism to quinoids, which are proposed to
A facile synthesis of 3-aryl-substituted-benzothiophenes via a Lewis acid mediated cyclization of 2-arylthio-acetophenones
Kim, Seongkon,Yang, Jane,DiNinno, Frank
, p. 2909 - 2912 (2007/10/03)
The boron trifluoride-etherate mediated cyclization of 2-arylthio- ketones 1a-h at ambient temperature gave 3-aryl-substituted benzothiophenes 2a-h in excellent yield. None of the rearranged 2-aryl-substituted benzothiophenes were observed.