81466-35-5Relevant academic research and scientific papers
EED-Targeted PROTACs Degrade EED, EZH2, and SUZ12 in the PRC2 Complex
Argyrou, Argyrides,Bagal, Sharan,Bednarski, Emma,Bloecher, Andrew,Castaldi, M. Paola,Chiarparin, Elisabetta,Code, Erin,Drew, Lisa,Fawell, Stephen,Gao, Ning,Hsu, Jessie Hao-Ru,Jacques, Kelly,Kawatkar, Sameer,O’ Donovan, Daniel H.,Pachl, Fiona,Rasmusson, Timothy,Rawlins, Philip,Read, Jon,Robinson, James,Shen, Minhui,Tomlinson, Ronald,Wilson, David M.,Woods, Haley,Zhu, Xiahui
, p. 41 - 46 (2020)
Deregulation of the PRC2 complex, comprised of the core subunits EZH2, SUZ12, and EED, drives aberrant hypermethylation of H3K27 and tumorigenicity of many cancers. Although inhibitors of EZH2 have shown promising clinical activity, preclinical data sugge
In silico and pharmacological screenings identify novel serine racemase inhibitors
Mori, Hisashi,Wada, Ryogo,Li, Jie,Ishimoto, Tetsuya,Mizuguchi, Mineyuki,Obita, Takayuki,Gouda, Hiroaki,Hirono, Shuichi,Toyooka, Naoki
supporting information, p. 3732 - 3735 (2014/09/03)
d-Serine is a coagonist of the N-methyl-d-aspartate (NMDA)-type glutamate receptor and its biosynthesis is catalyzed by serine racemase (SR). The overactivation of the NMDA receptor has been implicated in the development of neurodegenerative diseases, strokes, and epileptic seizures, thus, the inhibitors of SR have potential against these pathological states. Here, we have developed novel inhibitors of SR by in silico screening and in vitro enzyme assay. The newly developed inhibitors have lower IC50 value comparing with that of malonate, one of the standard SR inhibitor. The structural features of novel inhibitors suggest the importance of central amide structure having a phenoxy substituent in their structure for the SR inhibitory activity. The present findings suggest the importance and rational development of new drugs for diseases of NMDAR overactivation.
FUNCTIONALIZED DIPHENOLICS AND ABSORBABLE POLYMERS THEREFROM
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Page/Page column 20, (2008/06/13)
The present invention relates to dephenolic compounds, an example of which is shown below, which are functionalized, and polymers formed from the same. Polymers formed from the functionalized diphenolics are expected to have controllable degradation profiles, enabling them to release an active component over a desired time range. The polymers are also expected to be useful in a variety of medical applications.
Design and synthesis of potent and subtype-selective PPARα agonists
Desai, Ranjit C.,Metzger, Edward,Santini, Conrad,Meinke, Peter T.,Heck, James V.,Berger, Joel P.,MacNaul, Karen L.,Cai, Tian-Quan,Wright, Samuel D.,Agrawal, Arun,Moller, David E.,Sahoo, Soumya P.
, p. 1673 - 1678 (2007/10/03)
Beginning with a moderately potent PPARγ agonist 9, a series of potent and highly subtype-selective PPARα agonists was identified through a systematic SAR study. Based on the results of the efficacy studies in the hamster and dog models of dyslipidemia and the desired pharmacokinetic data, the optimized compound 39 was selected for further profiling.
Benzyloxy derivatives as MAOB inhibitors
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Page/Page column 9, (2008/06/13)
The invention relates to compounds of the formula and their pharmaceutically acceptable salts wherein R1, R2, R3, R4, R5, n, m, and o are as defined in the specification. The compounds are selective monoamine oxidase β inhibitors and are useful for the treatment and prevention of Alzheimer's disease and senile dementia, as well as other CNS disorders. The invention also relates to processes for preparing such compounds and pharmaceutical compositions containing them.
