title: Novel 3-Azaindolyl-4-arylmaleimides exhibiting potent antiangiogenic efficacy, protein kinase inhibition, and antiproliferative activity.
abstract: Tumor growth and metastasis are highly associated with the overexpression of protein kinases (PKs) regulating cell growth, apoptosis resistance, and prolonged cell survival. This study describes novel azaindolyl-maleimides with significant inhibition of PKs, such as VEGFR, FLT-3, and GSK-3β which are related to carcinogenesis. Furthermore, these compounds exhibit high kinase selectivity and potent inhibition of angiogenesis and cell proliferation, offering versatile options in cancer treatment strategies.
authors.affiliation: Department of Pharmacy, Johannes Gutenberg University of Mainz, Mainz, Germany.
authors.forename: Christopher
authors.initials: C
authors.lastname: Ganser
authors.forename: Eva
authors.initials: E
authors.lastname: Lauermann
authors.forename: Annett
authors.initials: A
authors.lastname: Maderer
authors.forename: Torsten
authors.initials: T
authors.lastname: Stauder
authors.forename: Jan-Peter
authors.initials: JP
authors.lastname: Kramb
authors.forename: Stanislav
authors.initials: S
authors.lastname: Plutizki
authors.forename: Thomas
authors.initials: T
authors.lastname: Kindler
authors.forename: Markus
authors.initials: M
authors.lastname: Moehler
authors.forename: Gerd
authors.initials: G
authors.lastname: Dannhardt
mesh_terms: D020533:Angiogenesis Inhibitors / Q000494:pharmacology*; D000818:Animals; D017209:Apoptosis / Q000187:drug effects; D002453:Cell Cycle / Q000187:drug effects; D049109:Cell Proliferation / Q000187:drug effects*; D002478:Cells, Cultured; D002642:Chick Embryo; D038362:Glycogen Synthase Kinase 3 / Q000037:antagonists & inhibitors; D000071679:Glycogen Synthase Kinase 3 beta; D006131:Growth Inhibitors / Q000494:pharmacology*; D061307:Human Umbilical Vein Endothelial Cells / Q000187:drug effects; D006801:Humans; D008301:Maleimides / Q000737:chemistry*; D015394:Molecular Structure; D009369:Neoplasms / Q000188:drug therapy*; D009389:Neovascularization, Pathologic / Q000188:drug therapy*; D047428:Protein Kinase Inhibitors / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D040301:Vascular Endothelial Growth Factor Receptor-2 / Q000037:antagonists & inhibitors; D040321:Vascular Endothelial Growth Factor Receptor-3 / Q000037:antagonists & inhibitors; D051941:fms-Like Tyrosine Kinase 3 / Q000037:antagonists & inhibitors
chemical_list: D020533:Angiogenesis Inhibitors; D006131:Growth Inhibitors; D008301:Maleimides; D047428:Protein Kinase Inhibitors; C043592:maleimide; C497970:FLT3 protein, human; D040301:Vascular Endothelial Growth Factor Receptor-2; D040321:Vascular Endothelial Growth Factor Receptor-3; D051941:fms-Like Tyrosine Kinase 3; C000605506:GSK3B protein, human; D000071679:Glycogen Synthase Kinase 3 beta; D038362:Glycogen Synthase Kinase 3