84807-37-4Relevant academic research and scientific papers
Discovery of a Selective and Potent Inhibitor of Mitogen-Activated Protein Kinase-Interacting Kinases 1 and 2 (MNK1/2) Utilizing Structure-Based Drug Design
Han, Wooseok,Ding, Yu,Xu, Yongjin,Pfister, Keith,Zhu, Shejin,Warne, Bob,Doyle, Mike,Aikawa, Mina,Amiri, Payman,Appleton, Brent,Stuart, Darrin D.,Fanidi, Abdallah,Shafer, Cynthia M.
, p. 3034 - 3045 (2016)
The discovery of a highly potent and selective small molecule inhibitor 9 for in vitro target validation of MNK1/2 kinases is described. The aminopyrazine benzimidazole series was derived from an HTS hit and optimized by utilization of a docking model, conformation analysis, and binding pocket comparison against antitargets.
Amine substituted N-(1H-benzimidazol-2ylmethyl)-5,6,7,8-tetrahydro-8-quinolinamines as CXCR4 antagonists with potent activity against HIV-1
Gudmundsson, Kristjan S.,Sebahar, Paul R.,Richardson, Leah D'Aurora,Miller, John F.,Turner, Elizabeth M.,Catalano, John G.,Spaltenstein, Andrew,Lawrence, Wendell,Thomson, Michael,Jenkinson, Stephen
scheme or table, p. 5048 - 5052 (2010/03/24)
Several novel amine substituted N-(1H-benzimidazol-2ylmethyl)-5,6,7,8-tetrahydro-8-quinolinamines were synthesized which had potent activity against HIV-1. The synthetic approaches adopted allowed for variation of the substitution pattern and resulting ch
2-Phenyl-4-piperazinylbenzimidazoles: Orally active inhibitors of the gonadotropin releasing hormone (GnRH) receptor
Pelletier, Jeffrey C.,Chengalvala, Murty,Cottom, Josh,Feingold, Irene,Garrick, Lloyd,Green, Daniel,Hauze, Diane,Huselton, Christine,Jetter, James,Kao, Wenling,Kopf, Gregory S.,Lundquist IV, Joseph T.,Mann, Charles,Mehlmann, John,Rogers, John,Shanno, Linda,Wrobel, Jay
, p. 6617 - 6640 (2008/12/22)
Antagonism of the gonadotropin releasing hormone (GnRH) receptor has shown positive clinical results in numerous reproductive tissue disorders such as endometriosis, prostate cancer and others. Traditional therapy has been limited to peptide agonists and
Chemical Compounds
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Page/Page column 19; 20, (2008/12/08)
The present invention provides compounds that demonstrate protective effects on target cells from HIV infection in a manner as to bind to a chemokine receptor, and which affect the binding of the natural ligand or chemokine to a receptor such as CXCR4 of
CHEMICAL COMPOUNDS
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Page/Page column 142, (2008/06/13)
The present invention provides compounds of Formula (I) comprising: including salts, solvates, and physiologically functional derivatives thereof, pharmaceutical formulations containing them, processes for their preparation, and methods of treatment using them.
CHEMICAL COMPOUNDS
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Page/Page column 193, (2010/10/20)
The present invention provides novel compounds that demonstrate protective effects on target cells from HIV infection in a manner as to bind specifically to the chemokine receptor, and which affect the binding of the natural ligand or chemokine to a receptor such as CXCR4 and/or CCR5 of a target cell.
