title: Design and synthesis of 3-(4,5,6,7-tetrahydro-3H-imidazo[4,5-c]pyridin-2-yl)-1H-quinolin-2-ones as VEGFR-2 kinase inhibitors.
abstract: A series of 3-(4,5,6,7-tetrahydro-3H-imidazo[4,5-c]pyridin-2-yl)-1H-quinolin-2-ones have been identified as a new class of VEGFR-2 kinase inhibitors. A variety of (4,5,6,7-tetrahydro-imidazo[5,4-c]pyridin-2-yl)-acetic acid ethyl esters were synthesized, and their VEGFR-2 inhibitory activity was evaluated. Described herein are the preparation of the series and the effects of the compounds on VEGFR-2 kinase activity.
authors.affiliation: Bio-Organic Science Division, Korea Research Institute of Chemical Technology, Daejeon, Republic of Korea.
authors.forename: Sun-Young
authors.initials: SY
authors.lastname: Han
authors.forename: Jie Won
authors.initials: JW
authors.lastname: Choi
authors.forename: Jeon
authors.initials: J
authors.lastname: Yang
authors.forename: Chong Hack
authors.initials: CH
authors.lastname: Chae
authors.forename: Jongkook
authors.initials: J
authors.lastname: Lee
authors.forename: Heejung
authors.initials: H
authors.lastname: Jung
authors.forename: Kwangho
authors.initials: K
authors.lastname: Lee
authors.forename: Jae Du
authors.initials: JD
authors.lastname: Ha
authors.forename: Hyoung Rae
authors.initials: HR
authors.lastname: Kim
authors.forename: Sung Yun
authors.initials: SY
authors.lastname: Cho
mesh_terms: D049109:Cell Proliferation / Q000187:drug effects; D002478:Cells, Cultured; D015195:Drug Design; D004789:Enzyme Activation / Q000187:drug effects; D006801:Humans; D007093:Imidazoles / Q000138:chemical synthesis / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D008958:Models, Molecular; D015394:Molecular Structure; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D011725:Pyridines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D015363:Quinolones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D040301:Vascular Endothelial Growth Factor Receptor-2 / Q000037:antagonists & inhibitors*
chemical_list: D007093:Imidazoles; D047428:Protein Kinase Inhibitors; D011725:Pyridines; D015363:Quinolones; D040301:Vascular Endothelial Growth Factor Receptor-2