274-95-3Relevant academic research and scientific papers
From Synthetic Simplified Marine Metabolite Analogues to New Selective Allosteric Inhibitor of Aurora B Kinase
Juillet, Charlotte,Ermolenko, Ludmila,Boyarskaya, Dina,Baratte, Blandine,Josselin, Béatrice,Nedev, Hristo,Bach, Stéphane,Iorga, Bogdan I.,Bignon, Jér?me,Ruchaud, Sandrine,Al-Mourabit, Ali
, p. 1197 - 1219 (2021/02/05)
Significant inhibition of Aurora B was achieved by the synthesis of simplified fragments of benzosceptrins and oroidin belonging to the marine pyrrole-2-aminoimidazoles metabolites isolated from sponges. Evaluation of kinase inhibition enabled the discovery of a synthetically accessible rigid acetylenic structural analogue EL-228 (1), whose structure could be optimized into the potent CJ2-150 (37). Here we present the synthesis of new inhibitors of Aurora B kinase, which is an important target for cancer therapy through mitosis regulation. The biologically oriented synthesis yielded several nanomolar inhibitors. The optimized compound CJ2-150 (37) showed a non-ATP competitive allosteric mode of action in a mixed-type inhibition for Aurora B kinase. Molecular docking identified a probable binding mode in the allosteric site "F"and highlighted the key interactions with the protein. We describe the improvement of the inhibitory potency and specificity of the novel scaffold as well as the characterization of the mechanism of action.
Organic compound comprising pyrimidine and organic electroluminescent device comprising the same
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Paragraph 0069; 0072; 0073; 0076; 0077, (2018/02/10)
The present invention relates to an organic aromatic organic compound containing pyridine, and an organic electroluminescent device using the same, wherein the compound may be used as thermally activated delayed fluorescent (TADF) material due to having little energy difference between an excited singlet state and an excited triplet state. Further, the compound of the present invention may be used in an organic light-emitting diode to improve efficiency of the organic light-emitting diode and lower driving voltage thereof.COPYRIGHT KIPO 2017
Azaindole Derivatives with High Affinity for the Dopamine D4 Receptor: Synthesis, Ligand Binding Studies and Comparison of Molecular Electrostatic Potential Maps
Loeber, Stefan,Huebner, Harald,Gmeiner, Peter
, p. 97 - 102 (2007/10/03)
Piperazinylmethyl substituted pyrazolopyridines and related heterocycles were synthesized and found to recognize selectivity the dopamine D4 receptor. For the most potent derivative 10d a Ki value of 2.0 nM was observed. SAR studies including the comparison of molecular isopotential surfaces were performed.
Synthesis and antibacterial activity of some imidazo[1,2-a[pyrimidine derivatives
Rival,Grassy,Michel
, p. 1170 - 1176 (2007/10/02)
A series of 75 imidazo[1,2-a]pyrimidine derivatives were synthesized. The 'in vitro' antibacterial activity of these compounds and their corresponding α-bromoketones against a variety of gram (+), gram (-) bacteria and Mycobacterium species is reported. Some of the prepared derivatives exhibited potent antimicrobial activity.
Antifungal activity in vitro of some imidazopyrimidine derivatives
Rival, Y,Grassy, G,Taudou, A,Ecalle, R
, p. 13 - 18 (2007/10/02)
In regard to fungicidal activity of imidazole ring found in chemical compounds such as econazole, a series of 42 diversely substituted imidazopyrimidines was synthetized and examined for its antifungal activity in several species.
