64132-13-4Relevant articles and documents
Supramolecular luminescent lanthanide dimers for fluoride sequestering and sensing
Liu, Tao,Nonat, Aline,Beyler, Maryline,Regueiro-Figueroa, Martín,Nchiminono, Katia,Jeannin, Olivier,Camerel, Franck,Debaene, Fran?ois,Cianférani-Sanglier, Sarah,Tripier, Rapha?l,Platas-Iglesias, Carlos,Charbonnière, Lo?c J.
, p. 7259 - 7263 (2014)
Lanthanide complexes (Ln=Eu, Tb, and Yb) that are based on a C 2-symmetric cyclen scaffold were prepared and characterized. The addition of fluoride anions to aqueous solutions of the complexes resulted in the formation of dinuclear supramolecular compounds in which the anion is confined into the cavity that is formed by the two complexes. The supramolecular assembly process was monitored by UV/Vis absorption, luminescence, and NMR spectroscopy and high-resolution mass spectrometry. The X-ray crystal structure of the europium dimer revealed that the architecture of the scaffold is stabilized by synergistic effects of the Eu-F-Eu bridging motive, πstacking interactions, and a four-component hydrogen-bonding network, which control the assembly of the two [EuL] entities around the fluoride ion. The strong association in water allowed for the luminescence sensing of fluoride down to a detection limit of 24nM.
Anticancer activity evaluation of indazolyl-substituted piperidin-4-yl-aminopyrimidines
Wang, Chao,Liu, Xiao-Wen,Xiao, Ting,Xu, Zhi-Qiang,Cao, Shuang,Wang, Hai-Feng,Yan, Qiong-Jiao,Gu, Shuang-Xi,Zhu, Yuan-Yuan
, p. 910 - 915 (2020)
Based on our previous work, a series of indazolyl-substituted piperidin-4-yl-aminopyrimidines, which were firstly used as anti-HIV agents, were evaluated for their anticancer potency in five cancer cell lines. Notably, they exhibited excellent activities
Implementation of the CYP Index for the Design of Selective Tryptophan-2,3-dioxygenase Inhibitors
Castanedo, Georgette M.,Dement, Kevin,Dipasquale, Antonio,Gazzard, Lewis,Goon, Leanne,Gustafson, Amy,Harris, Seth F.,Jaipuri, Firoz A.,Kumar, Sanjeev,La, Hank,Li, Xiaokai,Liu, Wen,Liu, Yichin,Mautino, Mario R.,Mendonca, Rohan,Oh, Angela J.,Parr, Brendan T.,Pastor, Richard,Pavana, Roheeth K.,Pei, Zhonghua,Potturi, Hima,Sellers, Benjamin D.,Shao, Cheng,Vanderporten, Erica C.,Velvadapu, Venkata,Waldo, Jesse P.,Wu, Guosheng,Yuen, Po-Wai,Zhang, Yamin,Zhang, Zuhui
supporting information, p. 541 - 549 (2020/04/30)
A class of imidazoisoindole (III) heme-binding indoleamine-2,3-dioxygenase (IDO1) inhibitors were optimized via structure-based drug design into a series of tryptophan-2,3-dioxygenase (TDO)-selective inhibitors. Kynurenine pathway modulation was demonstrated in vivo, which enabled evaluation of TDO as a potential cancer immunotherapy target. As means of mitigating the risk of drug-drug interactions arising from cytochrome P450 inhibition, a novel property-based drug design parameter, herein referred to as the CYP Index, was implemented for the design of inhibitors with appreciable selectivity for TDO over CYP3A4. We anticipate the CYP Index will be a valuable design parameter for optimizing CYP inhibition of any small molecule inhibitor containing a Lewis basic motif capable of binding heme.
EPHA4 CYCLIC PEPTIDE ANTAGONISTS AND METHODS OF USE THEREOF
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, (2019/11/19)
Disclosed herein are compounds and methods of use thereof for the modulation of EphA4 receptor activity. In an aspect, is provided a method of treating or preventing a disease or disorder mediated by EphA4, comprising administering to a subject in need thereof a therapeutically effective amount of a compound as described herein, including certain embodiments, or the structural Formula (I), (l-A), (II), (III), (IV), (IV-1), (V), (Vl-A), (Vl-B), (VII-1), (VII-2), (VIII-1), or (VIII-2), or an enantiomer, a mixture of enantiomers, a mixture of two or more diastereomers, or an isotopic variant thereof; or a pharmaceutically acceptable salt, solvate, or hydrate thereof.