8 research outputs found
Design and Synthesis of 5,6-fused Heterocyclic Amides as Raf Kinase Inhibitors
Two novel scaffolds based on 5,6-fused heterocyclic backbones were designed and synthesized as Raf kinase inhibitors. The scaffolds were assessed for in vitro pan-Raf inhibition, activity in cell proliferation and target modulation assays, and pharmacokinetic parameters
Discovery of A Selective and Potent Inhibitor of MNK Kinase 1/2 Utilizing Structure-Based Drug Design
The discovery of a highly potent and selective small molecule inhibitor 8 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 anti-targets
Discovery of a Selective and Potent Inhibitor of Mitogen-Activated Protein Kinase-Interacting Kinases 1 and 2 (MNK1/2) Utilizing Structure-Based Drug Design
The discovery of a highly potent
and selective small molecule inhibitor <b>9</b> 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
Discovery of a Selective and Potent Inhibitor of Mitogen-Activated Protein Kinase-Interacting Kinases 1 and 2 (MNK1/2) Utilizing Structure-Based Drug Design
The discovery of a highly potent
and selective small molecule inhibitor <b>9</b> 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