1. Academic Validation
  2. 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

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

  • Eur J Med Chem. 2007 Nov-Dec;42(11-12):1317-24. doi: 10.1016/j.ejmech.2007.02.007.
Simone Kohfeld 1 Peter G Jones Frank Totzke Christoph Schächtele Michael H G Kubbutat Conrad Kunick
Affiliations

Affiliation

  • 1 Technische Universität Braunschweig, Institut für Pharmazeutische Chemie, Beethovenstrasse 55, D-38106 Braunschweig, Germany.
Abstract

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.

Figures