796844-14-9Relevant articles and documents
Identification of New Small-Molecule Inducers of Estrogen-related Receptor α (ERRα) Degradation
Peng, Lijie,Zhang, Zhensheng,Lei, Chong,Li, Shan,Zhang, Zhang,Ren, Xiaomei,Chang, Yu,Zhang, Yan,Xu, Yong,Ding, Ke
, p. 767 - 772 (2019)
A series of (E)-3-(4-((2,4-bis(trifluoromethyl)benzyl)oxy)-3-methoxyphenyl)-2-cyanoacrylamide derivatives were designed and synthesized as new estrogen-related receptor α (ERRα) degraders based on the proteolysis targeting chimera (PROTAC) concept. One of the representative compounds 6c is capable of specifically degrading ERRα protein by >80% at a relatively low concentration of 30 nM, becoming one of the most potent and selective ERRα degraders to date. Compound 6c could be utilized as a new powerful research tool for further biological investigation of ERRα.
PHENYL [A]INDOLE[2,3-G]QUINOLIZINE COMPOUNDS, PREPARATION METHOD THEREFOR, PHARMACEUTICAL COMPOSITION, AND APPLICATIONS THEREOF
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Paragraph 0062, (2019/02/13)
The present invention relates to phenyl [a]indole[2,3-g]quinolizine compounds represented by formula (I), a preparation method therefor, a pharmaceutical composition, and applications thereof. Specific applications are applications in the preparation of d
PHARMACEUTICAL COMPOSITIONS
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Page/Page column 41, (2008/06/13)
Compounds for use in compositions and methods for modulating the activity of nuclear receptors are provided. In particular, compounds for use in compositions and methods for modulating the estrogen related receptors are provided. In one embodiment, the compounds provided herein are ERR modulators. In another embodiment, the compounds provided herein are agonists, partial agonists, antagonists. or inverse agonists of ERR or ERR?. In certain embodiments, the compounds of the invention, as described above in the Summary of the Invention, are compounds of formula (I).