849068-61-7Relevant academic research and scientific papers
HETEROARYL COMPOUNDS AS NECROSIS INHIBITORS, COMPOSITION AND METHOD USING THE SAME
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Paragraph 00146; 00149-00150, (2020/07/25)
The present disclosure provides heteroaryl compounds of Formula (I), processes for their preparation, pharmaceutical compositions containing them, and their use in the treatment of diseases and disorders, arising from or related to necrosis. Formula (I) i
Structural Optimization and Pharmacological Evaluation of Inhibitors Targeting Dual-Specificity Tyrosine Phosphorylation-Regulated Kinases (DYRK) and CDC-like kinases (CLK) in Glioblastoma
Zhou, Qingqing,Phoa, Athena F.,Abbassi, Ramzi H.,Hoque, Monira,Reekie, Tristan A.,Font, Josep S.,Ryan, Renae M.,Stringer, Brett W.,Day, Bryan W.,Johns, Terrance G.,Munoz, Lenka,Kassiou, Michael
, p. 2052 - 2070 (2017/03/17)
The DYRK family contains kinases that are up-regulated in malignancy and control several cancer hallmarks. To assess the anticancer potential of inhibitors targeting DYRK kinases, we developed a series of novel DYRK inhibitors based on the 7-azaindole scaffold. All compounds were tested for their ability to inhibit DYRK1A, DYRK1B, DYRK2, and the structurally related CLK1. The library was screened for anticancer efficacy in established and stem cell-like glioblastoma cell lines. The most potent inhibitors (IC50 ≤ 50 nM) significantly decreased viability, clonogenic survival, migration, and invasion of glioblastoma cells. Target engagement was confirmed with genetic knockdown and the cellular thermal shift assay. We demonstrate that DYRK1A’s thermal stability in cells is increased upon compound treatment, confirming binding in cells. In summary, we present synthesis, structure-activity relationship, and efficacy in glioblastoma-relevant models for a library of novel 7-azaindoles.
Compounds used as JAK inhibitor, and use of compounds
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Paragraph 0557; 0558; 0559, (2017/08/27)
The invention provides compounds used as a JAK inhibitor, and a use of the compounds, and concretely provides compounds (represented by formula (I)) with JAK inhibition activity or a stereoisomer, a geometric isomer, a tautomer, a racemate, a nitrogen oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, and a medicinal composition including the compounds. The invention also discloses a use of the compounds or the medicinal composition thereof in the preparation of medicines used for treating autoimmune diseases or proliferative diseases.
NOVEL INHIBITORS HEPATITIS C VIRUS REPLICATION
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Page/Page column 287; 290, (2008/12/08)
The embodiments provide compounds of the general Formula I, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus
NEW DERIVATIVES OF 5-ARYL-1H-PYRROLO [2, 3B] PYRIDINE-3-CARBOXAMIDE OR 5-ARYL-1H-PYRROLO [2, 3B] PYRIDINE-3-CARBOXYLIC ACID
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Page/Page column 21-22, (2008/06/13)
The present invention relates to new compounds of formula I as a free base or a pharmaceutically acceptable salt, solvate or solvate of salt thereof, a process for their preparation and new intermediates used therein, pharmaceutical formulations containin
COMPOSITIONS USEFUL AS INHIBITORS OF PROTEIN KINASES
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Page/Page column 182-183, (2010/02/11)
The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
