Synthesis and structure-activity relationships of 1,2,3,4-tetrahydropyrido[2,3-b]pyrazines as potent and selective inhibitors of the anaplastic lymphoma kinase.
Milkiewicz, Karen L; Weinberg, Linda R; Albom, Mark S; Angeles, Thelma S; Cheng, Mangeng; Ghose, Arup K; Roemmele, Renee C; Theroff, Jay P; Underiner, Ted L; Zificsak, Craig A; Dorsey, Bruce D.
Bioorg Med Chem
; 18(12): 4351-62, 2010 Jun 15.
Artigo em Inglês | MEDLINE | ID: mdl-20483621
Discovery of a potent tyrosine kinase AXL inhibitor bearing the 3-((2,3,4,5-tetrahydro-1H-benzo[d]azepin-7-yl)amino)pyrazine core.
Synthetic, Structural, and Anticancer Activity Evaluation Studies on Novel Pyrazolylnucleosides.
Addressing Kinase-Independent Functions of Fak via PROTAC-Mediated Degradation.
Discovery of 2,6-disubstituted pyrazine derivatives as inhibitors of CK2 and PIM kinases.
Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors.
Discovery of a novel aminopyrazine series as selective PI3Kα inhibitors.
Structure-based design of imidazo[1,2-a]pyrazine derivatives as selective inhibitors of Aurora-A kinase in cells.
Novel 3-arylethynyl-substituted thieno[3,4-b]pyrazine derivatives as human transglutaminase 2 inhibitors.
In vivo optimization of 2,3-diaminopyrazine Rho Kinase inhibitors for the treatment of glaucoma.
Design, synthesis, and biological evaluation of new pyrazino[1,2-a]benzimidazole derivatives as selective cyclooxygenase (COX-2) inhibitors.