Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 56, Issue -, Pages 246-253Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2012.08.022
Keywords
Tetrahydroazepinone; Hymenialdisine; Kenpaullone; Marine natural products; Oximes
Categories
Funding
- Welsh Office for Research and Development (WORD)
Ask authors/readers for more resources
The tetrahydroazepinone pharmacophore is a component of many interesting compounds, including several marine natural products, with anti-cancer properties. The synthesis and biological evaluation of a novel series of pyrroloazepinone and indoloazepinone oximes is reported. These compounds showed promising growth inhibition activity against four human cancer cell lines but did not significantly inhibit the cell cycle regulator cyclin dependent kinase 2. The most active compounds in this series displayed improved anti-proliferative activity over the related synthetic indoloazepine kenpaullone. The structure activity relationships exhibited by the azepinone pharmacophore suggests several novel lead compounds for anti-cancer drug discovery. Crown Copyright (C) 2012 Published by Elsevier Masson SAS. All rights reserved.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available