50820-64-9Relevant academic research and scientific papers
Tritopic Triazatruxene Ligands for Multicomponent Metal-Organic Frameworks
Alka?, Adil,Cornelio, Joel,Telfer, Shane G.
, p. 1167 - 1174 (2019)
Multicomponent metal-organic frameworks (MOFs) are built up from multiple ligands that are geometrically distinct. These ligands occupy specific positions in the MOF lattice. Installing different functionalities at precise locations in the framework is an important step in making MOFs for specific applications. This can be achieved by designing functionalized ligands for multicomponent MOFs. Here, we report a simple synthetic procedure for a new tritopic triazatruxene based tricarboxylic acid, H3tat. We show that this ligand can be symmetrically derivatized with various substituents on its nitrogen centres. We report a new isoreticular series of well-ordered quaternary MOFs based on these new triazatruxene ligands together with two linear carboxylate ligands and Zn4O clusters. These MOFs are isostructural to the previously reported MUF-77 series and show similar high surface areas and large pore volumes. Furthermore, H-bonding between the NH sites of the incorporated triazatruxene ligands and guest molecules is employed to modify their fluorescence behavior.
Early Drug-Discovery Efforts towards the Identification of EP300/CBP Histone Acetyltransferase (HAT) Inhibitors
Audia, James E.,Bommi-Reddy, Archana,Brucelle, Francois,Cantone, Nico,Cummings, Richard,Gardberg, Anna S.,Huhn, Annissa J.,Levell, Julian,Patel, Chirag,Patel, Gaurav,Poy, Florence,Sims, Robert,Vivat, Valerie,Wilson, Jonathan E.
supporting information, (2020/04/20)
EP300 and CBP (KAT3A/3B) are two highly homologous, multidomain, epigenetic coregulators that play central roles in transcription through the acetylation of lysine residues on histones and other proteins. Both enzymes have been implicated in human diseases, especially cancer. From a high-throughput screen of 191 000 compounds searching for EP300/CBP histone acetyltransferase (HAT) inhibitors, 18 compounds were characterized by a suite of biochemical enzymatic assays and biophysical methods, including X-ray crystallography and native mass spectrometry. This work resulted in the discovery of three distinct mechanistic classes of EP300/CBP HAT inhibitors, including two classes not previously described. The profiles of an example of each class of inhibitor are described in detail. A subsequent medicinal chemistry effort led to the development of a novel class of orally bioavailable AcCoA-competitive EP300/CBP HAT inhibitors with in vivo activity. We believe that this work will prove to be a useful guide for other groups interested in the development of HAT inhibitors.
Discovery and structure-activity relationship studies of N-substituted indole derivatives as novel Mcl-1 inhibitors
Luan, Shenglin,Ge, Qi,Chen, Yedong,Dai, Mingyang,Yang, Jinyu,Li, Kun,Liu, Dan,Zhao, Linxiang
supporting information, p. 1943 - 1948 (2017/04/07)
Myeloid cell leukemia-1 (Mcl-1) is an important antiapoptotic protein functioning through protein-protein interactions. We discovered LSL-A6 (2-((2-carbamoyl-1-(3-(4-methoxyphenoxy)propyl)-1H-indol-6-yl)oxy)acetic acid) with a novel N-substituted indole scaffold to interfere Mcl-1 binding as a novel Mcl-1 inhibitor. Molecular modeling indicated that this compound binds with Mcl-1 by interaction with P2 and R263 hot-spots. Structure modification focused on several moieties including indole core, hydrophobic tail and acidic chain were conducted and structure-activity relationship was analyzed. The most potent compound 24d which exhibited Ki value of 110?nM for interfering Mcl-1 binding was obtained after hit-to-lead modification.
N-substituted indole derivative and application thereof
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Paragraph 0341; 0342, (2017/08/28)
The invention belongs to the technical field of medicine, and relates to an N-substituted indole derivative, pharmaceutically acceptable salts and hydrates thereof, a pharmaceutical composition taking the derivative as an active component, and application
N-(2-ARYLETHYL) BENZYLAMINES AS ANTAGONISTS OF THE 5-HT6 RECEPTOR
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Paragraph 0177, (2016/01/25)
The present invention relates to the use compounds of formula I which are antagonists of the 5-HT 6 receptor, for treating a cognitive disorder selected from the group consisting of age-related cognitive decline, mild cognitive impairment and dementia
THIOHYDROXAMATES AS INHIBITORS OF HISTONE DEACETYLASE
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Page/Page column 90, (2009/02/11)
Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of histone deacetylase. Also described herein are methods of using such HDAC inhibitors, alone and in combination with other compounds, fo
Novel indole inhibitors of IMPDH from fragments: Synthesis and initial structure-activity relationships
Beevers, Rebekah E.,Buckley, George M.,Davies, Natasha,Fraser, Joanne L.,Galvin, Francis C.,Hannah, Duncan R.,Haughan, Alan F.,Jenkins, Kerry,Mack, Stephen R.,Pitt, William R.,Ratcliffe, Andrew J.,Richard, Marianna D.,Sabin, Verity,Sharpe, Andrew,Williams, Sophie C.
, p. 2539 - 2542 (2007/10/03)
The elaboration of previously reported indole fragments as inhibitors of inosine monophosphate dehydrogenase (IMPDH) is described. The synthesis, in vitro inhibitory values for IMPDH II, PBMC proliferation and physicochemical properties are discussed.
Pyrrole-2,3-quinodimethane Analogues in the Synthesis of Indoles. Part 2. Synthesis and Diels-Alder Reactions of 1,6-Dihydropyranopyrrol-6(1H)-ones
Andrews, John F. P.,Jackson, P. Mark,Moody, Christopher J.
, p. 7353 - 7372 (2007/10/02)
The pyranopyrrol-6-ones 7-9, 12 and 13 are stable cyclic analogues of pyrrole-2,3-quinodimethane, and undergo Diels-Alder reaction with a range of alkynes to give, after loss of carbon dioxide, indoles.
