882188-87-6Relevant academic research and scientific papers
Indazolyl-substituted piperidin-4-yl-aminopyrimidines as HIV-1 NNRTIs: Design, synthesis and biological activities
Xiao, Ting,Tang, Jia-Fan,Meng, Ge,Pannecouque, Christophe,Zhu, Yuan-Yuan,Liu, Gen-Yan,Xu, Zhi-Qiang,Wu, Feng-Shou,Gu, Shuang-Xi,Chen, Fen-Er
, (2019/12/09)
A series of indazolyl-substituted piperidin-4-yl-aminopyrimidines (IPAPYs) were designed from two potent HIV-1 NNRTIs piperidin-4-yl-aminopyrimidine 3c and diaryl ether 4 as the lead compounds by molecular hybridization strategy. The target molecules 5a-q
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 (2020/03/26)
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
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.
[6,6] FUSED BICYCLIC HDAC8 INHIBITORS
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, (2019/08/15)
The present invention is directed to compounds of Formula I: and pharmaceutically acceptable salts, prodrugs, solvates, hydrates, tautomers, or isomers or thereof, wherein R1, R2, R2', L, X, W, Y1,Y2,
A process for preparing 1 - tert-butoxycarbonyl - 3 - hydroxy methyl indazole method and application
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Paragraph 0027; 0028; 0033; 0034; 0038; 0039; 0043; 0044, (2017/08/26)
The invention discloses a method for preparing 1-tert-butoxy carbonyl-3-hydroxymethyl indazole in a large scale. The method comprises the following steps: protecting amino by using tert-butoxy carbonyl (Boc) by taking 3-indazole formic ether as the starting raw material, and reducing an ester group into alcohol by adopting sodium borohydride and a catalyst at room temperature so as to obtain the 1-tert-butoxy carbonyl-3-hydroxymethyl indazole. The method disclosed by the invention is cheap, moderate in reaction condition, simple in operation process and simple and convenient to post-process; a reaction reagent is easy to obtain; the purity and the yield of the 1-tert-butoxy carbonyl-3-hydroxymethyl indazole are high; the method is applied to industrial large-scale production and the like; and the 1-tert-butoxy carbonyl-3-hydroxymethyl indazole prepared by the invention can be used for preparing a compound having biological activity.
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 (2014/07/21)
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.
Identification of a buried pocket for potent and selective inhibition of Chk1: Prediction and verification
Foloppe, Nicolas,Fisher, Lisa M.,Francis, Geraint,Howes, Rob,Kierstan, Peter,Potter, Andrew
, p. 1792 - 1804 (2007/10/03)
Inhibition of the Chk1 kinase by small molecules binding to its active site is a strategy of great therapeutic interest for oncology. We report how computational modelling predicted the binding mode of ligands of special interest to the Chk1 ATP site, for representatives of an indazole series and debromohymenialdisine. These binding modes were subsequently confirmed by X-ray crystallography. The binding mode of a potent indazole derivative involves non-conventional C-H...O and N-H...π-aromatic interactions with the protein. These interactions are formed in a buried pocket at the periphery of the ATP-binding site, the importance of which has previously been overlooked for ligand design against Chk1. It is demonstrated that filling this pocket can confer ligands with dramatically enhanced affinity for Chk1. Structural arguments in conjunction with assay data explain why targeting this pocket is also advantageous for selective binding to Chk1. Structural overlays of known inhibitors complexed with Chk1 show that only the indazole series utilizes the pocket of interest. Therefore, the analysis presented here should prove helpful in guiding future structure-based ligand design efforts against Chk1.
