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

Simone Kohfeld; Peter G Jones; Frank Totzke; Christoph Schächtele; Michael H G Kubbutat; Conrad Kunick

doi:10.1016/j.ejmech.2007.02.007

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. Epub 2007 Mar 1.

Authors

Simone Kohfeld¹, Peter G Jones, Frank Totzke, Christoph Schächtele, Michael H G Kubbutat, Conrad Kunick

Affiliation

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

PMID: 17448574
DOI: 10.1016/j.ejmech.2007.02.007

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Benzazepines / chemical synthesis*
Benzazepines / chemistry
Benzazepines / pharmacology*
Breast Neoplasms / enzymology
Breast Neoplasms / pathology*
Cell Line, Tumor
Cell Proliferation / drug effects
Computational Biology
Humans
Indoles / chemistry
Indoles / pharmacology
Inhibitory Concentration 50
Leukemia / enzymology
Leukemia / pathology*
Protein Kinase Inhibitors / chemistry

Substances

Benzazepines
Indoles
Protein Kinase Inhibitors
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