17106-13-7Relevant academic research and scientific papers
Screening of a Custom-Designed Acid Fragment Library Identifies 1-Phenylpyrroles and 1-Phenylpyrrolidines as Inhibitors of Notum Carboxylesterase Activity
Mahy, William,Patel, Mikesh,Steadman, David,Woodward, Hannah L.,Atkinson, Benjamin N.,Svensson, Fredrik,Willis, Nicky J.,Flint, Alister,Papatheodorou, Dimitra,Zhao, Yuguang,Vecchia, Luca,Ruza, Reinis R.,Hillier, James,Frew, Sarah,Monaghan, Amy,Costa, Artur,Bictash, Magda,Walter, Magnus W.,Jones, E. Yvonne,Fish, Paul V.
, p. 9464 - 9483 (2020/10/19)
The Wnt family of proteins are secreted signaling proteins that play key roles in regulating cellular functions. Recently, carboxylesterase Notum was shown to act as a negative regulator of Wnt signaling by mediating the removal of an essential palmitoleate. Here we disclose two new chemical scaffolds that inhibit Notum enzymatic activity. Our approach was to create a fragment library of 250 acids for screening against Notum in a biochemical assay followed by structure determination by X-ray crystallography. Twenty fragments were identified as hits for Notum inhibition, and 14 of these fragments were shown to bind in the palmitoleate pocket of Notum. Optimization of 1-phenylpyrrole 20, guided by structure-based drug design, identified 20z as the most potent compound from this series. Similarly, the optimization of 1-phenylpyrrolidine 8 gave acid 26. This work demonstrates that inhibition of Notum activity can be achieved by small, drug-like molecules possessing favorable in vitro ADME profiles.
BORON-CONTAINING CYCLIC EMISSIVE COMPOUNDS AND COLOR CONVERSION FILM CONTAINING THE SAME
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, (2020/10/21)
The present disclosure relates to novel photoluminescent complexes comprising a BODIPY moiety covalently bonded to a blue light absorbing moiety, a color conversion film comprising the photoluminescent complex, and a back-light unit using the same.
NOVEL PROCESS
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Page/Page column 45-46, (2010/04/03)
The present invention relates to novel intermediates and further to the use of said intermediates in processes for the preparation of indolinone derivatives, in particular 3- pyrrole substituted 2-indolinones having amide moieties on the pyrrole ring. Such compounds are useful in die treatment of abnormal cell growth, such as cancer, in mammals.
Development of 2,6-carboxy-substituted boron dipyrromethene (BODIPY) as a novel scaffold of ratiometric fluorescent probes for live cell imaging
Komatsu, Toru,Urano, Yasuteru,Fujikawa, Yuuta,Kobayashi, Tomonori,Kojima, Hirotatsu,Terai, Takuya,Hanaoka, Kenjiro,Nagano, Tetsuo
supporting information; experimental part, p. 7015 - 7017 (2010/04/25)
Ratiometric fluorescent probes based on boron dipyrromethene (BODIPY) were developed based on a novel design strategy, in which a change of the electron-withdrawing character of the 2,6-substituents resulting from reaction with a target molecule generates a fluorescence wavelength change. The Royal Society of Chemistry 2009.
