50365-34-9Relevant academic research and scientific papers
Discovery of an MLLT1/3 YEATS Domain Chemical Probe
Moustakim, Moses,Christott, Thomas,Monteiro, Octovia P.,Bennett, James,Giroud, Charline,Ward, Jennifer,Rogers, Catherine M.,Smith, Paul,Panagakou, Ioanna,Díaz-Sáez, Laura,Felce, Suet Ling,Gamble, Vicki,Gileadi, Carina,Halidi, Nadia,Heidenreich, David,Chaikuad, Apirat,Knapp, Stefan,Huber, Kilian V. M.,Farnie, Gillian,Heer, Jag,Manevski, Nenad,Poda, Gennady,Al-awar, Rima,Dixon, Darren J.,Brennan, Paul E.,Fedorov, Oleg
supporting information, p. 16302 - 16307 (2018/11/23)
YEATS domain (YD) containing proteins are an emerging class of epigenetic targets in drug discovery. Dysregulation of these modified lysine-binding proteins has been linked to the onset and progression of cancers. We herein report the discovery and characterisation of the first small-molecule chemical probe, SGC-iMLLT, for the YD of MLLT1 (ENL/YEATS1) and MLLT3 (AF9/YEATS3). SGC-iMLLT is a potent and selective inhibitor of MLLT1/3–histone interactions. Excellent selectivity over other human YD proteins (YEATS2/4) and bromodomains was observed. Furthermore, our probe displays cellular target engagement of MLLT1 and MLLT3. The first small-molecule X-ray co-crystal structures with the MLLT1 YD are also reported. This first-in-class probe molecule can be used to understand MLLT1/3-associated biology and the therapeutic potential of small-molecule YD inhibitors.
Synthesis and evaluation of benzimidazole derivatives as selective COX-2 inhibitors
Rathore, Ankita,Mujeeb-Ur-Rahman,Siddiqui, Anees A.,Ali, Abuzer,Yar, Mohammad Shahar
, p. 188 - 199 (2015/04/14)
A new series of 1-{(5-substituted-alkyl/aryl-1,3,4-oxadiazol-2-yl)methyl}-2-(piperidin-1-ylmethyl)-1Hbenzimidazoles (5a-5r) was synthesized and screened for their inhibitory activity against COX (1 and 2). In vivo antiinflammatory activity of potent compounds was done by carrageenan-induced rat paw edema model. In vitro anticancer activity of synthesized compounds was also performed at the National Cancer Institute (NCI) against NCI 60 cell lines panel. Out of the 18 compounds screened, 5h, 5i, 5j and 5l were found to be potent COX-2 inhibitors in the range of IC50 0.06-0.81 μM. In vivo anti-inflammatory screening results revealed that the compounds 5h and 5j manifested profound percent protection of 72.8 and 75.0%, respectively. Compound 5f exhibited moderate cytotoxicity with 58.79% growth inhibition against SNB-75 (CNS Cancer) cell lines and moderate activity against COX-2 (IC50 = 8.0 μM).
BENZIMIDAZOLE DERIVATIVES AS SELECTIVE BLOCKERS OF PERSISTENT SODIUM CURRENT
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Page/Page column 30, (2013/07/19)
The present invention is directed to methods of treating diseases or conditions mediated by elevated persistent sodium channel, such as ocular disorders, pain, multiple sclerosis, and seizure disorders utilizing a compound of Formula I or a pharmaceutically acceptable salt thereof or a pharmaceutical composition comprising said compound, wherein variables R, R1, R2, R3, R4, R5, m, and n in Formula I are as defined herein
Tailored ligand acceleration of the cu-catalyzed azide-alkyne cycloaddition reaction: Practical and mechanistic implications
Presolski, Stanislav I.,Hong, Vu,Cho, So-Hye,Finn
supporting information; experimental part, p. 14570 - 14576 (2010/12/24)
Tris(heterocyclemethyl)amines containing mixtures of 1,2,3-triazolyl, 2-benzimidazoyl, and 2-pyridyl components were prepared for ligand acceleration of the copper-catalyzed azide-alkyne cycloaddition reaction. Two classes of ligands were identified: thos
