97725-08-1Relevant articles and documents
Synthesis of Emissive Heteroacene Derivatives via Nucleophilic Aromatic Substitution
Hiscock, Lana K.,Yao, Chengzhang,Skene,Dawe, Louise N.,Maly, Kenneth E.
, p. 15530 - 15537 (2019)
A synthetic approach for preparing a variety of heterocyclic tetrahydropentacene derivatives via nucleophilic aromatic substitution reactions of bidentate nucleophiles and tetrafluoroterephthalonitrile was developed. X-ray crystallography of several products revealed that the compounds containing oxygen and nitrogen heteroatoms are highly planar and engage in π-stacking, while the compounds containing sulfur are bent and do not stack as effectively. The compounds were also highly emissive, and the heteroatom had a significant impact on the emission and electrochemical properties.
RESIN COMPOSITION
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Paragraph 0184, (2019/08/18)
The present invention provides a resin composition having a high sensitivity and serving to produce a cured film with a low water absorption rate. The resin composition includes: (a) an alkali-soluble resin and (b1) an amido-phenol compound containing a p
Analysis of chain length, substitution patterns, and unsaturation of AM-404 derivatives as 20S proteasome stimulators
Coleman, Rachel A.,Muli, Christine S.,Zhao, Yizhou,Bhardwaj, Atul,Newhouse, Timothy R.,Trader, Darci J.
supporting information, p. 420 - 423 (2019/01/04)
Proteasome-mediated degradation of proteins is a vital cellular process and is performed by the ubiquitin-dependent proteasome system (UPS) and the ubiquitin-independent proteasome system (UIPS). While both systems are necessary to maintain healthy cell function, many disease states are characterized by reduced activity of the UPS, and the UIPS cannot by itself maintain proper protein levels. It has been suggested that the 20S core particle (20S CP), the isoform of the proteasome in the UIPS that can degrade proteins without a ubiquitin tag, can be stimulated with a small molecule to assist the 20S CP to accept and hydrolyze substrates more rapidly. Several small molecule stimulators of the 20S CP have since been discovered, including AM-404, an arachidonic acid derivative. AM-404 has previously been shown to inhibit fatty acid amide hydrolase activity. We wished to evaluate what structural components of AM-404 are required to stimulate the 20S CP with the long-term goal of using this information to design a stimulator with better drug-like qualities. We synthesized numerous derivatives of AM-404, varying the chain length, substitutions, and degree of unsaturation. Through this endeavor, we obtained several molecules capable of stimulating the 20S CP to various degrees. We discovered that though chain length is important, the presence of a cis-alkene in a specific location in the aliphatic chain has the greatest impact on the ability to stimulate the 20S CP. Two of the derivatives maintain modest stimulatory activity, and have improved toxicity over AM-404.
