1-Aryl-4,6-dihydropyrazolo[4,3-d][1]benzazepin-5(1H)-ones: a new class of antiproliferative agents with selectivity for human leukemia and breast cancer cell lines.
The synthesis of 1-aryl-4,6-dihydropyrazolo[4,3-d][1]benzazepin-5(1H)-ones by cyclization of 4-[(dimethylamino)methylidene]-3,4-dihydro-1H-[1]benzazepine-2,5-dione with arylhydrazines is reported. When tested on a panel of human cancer cell lines, the title compounds showed antiproliferative activity and a characteristic selectivity pattern of growth inhibition. Although structurally akin to established kinase inhibitors, the new compounds did not exhibit noteworthy inhibitory activity when tested on an array of cancer-related kinases.
Kohfeld
Simone
S
Technische Universität Braunschweig, Institut für Pharmazeutische Chemie, Beethovenstrasse 55, D-38106 Braunschweig, Germany.
Jones
Peter G
PG
Totzke
Frank
F
Schächtele
Christoph
C
Kubbutat
Michael H G
MH
Kunick
Conrad
C
D001552:Benzazepines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001943:Breast Neoplasms / Q000201:enzymology / Q000473:pathology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D019295:Computational Biology; D006801:Humans; D007211:Indoles / Q000737:chemistry / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D007938:Leukemia / Q000201:enzymology / Q000473:pathology*; D047428:Protein Kinase Inhibitors / Q000737:chemistry
D001552:Benzazepines; D007211:Indoles; D047428:Protein Kinase Inhibitors; C120793:alsterpaullone