Ferrocenyl chalcone difluoridoborates inhibit HIV-1 integrase and display low activity towards cancer and endothelial cells.

Abstract

We report here the discovery of a potent series of HIV-1 integrase (IN) inhibitors based on the ferrocenyl chalcone difluoridoborate structure. Ten new compounds have been synthesized and were generally found to have similar inhibitory activities against the IN 3' processing and strand transfer (ST) processes. IC(50) values were found to be in the low micromolar range, and significantly lower than those found for the non-coordinated ferrocenyl chalcones and other ferrocene molecules. The ferrocenyl chalcone difluoridoborates furthermore exhibited low cytotoxicity against cancer cells and low morphological activity against epithelial cells.

• Authors: Jean-Philippe Monserrat, Rasha I Al-Safi, Keshri Nath Tiwari, Lionel Quentin, Guy G Chabot, Anne Vessières, Gérard Jaouen, Nouri Neamati, Elizabeth A Hillard
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 21 Issue 20 Pg. 6195-7 (Oct 15 2011) ISSN: 1464-3405 [Electronic] England
• PMID: 21889342 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: Copyright © 2011 Elsevier Ltd. All rights reserved.

Chemical References

• Borates
• Chalcones
• HIV Integrase Inhibitors
• Chalcone
• HIV Integrase
• p31 integrase protein, Human immunodeficiency virus 1

Topics

• Borates (chemistry, pharmacology)
• Cell Line, Tumor
• Chalcone
• Chalcones (chemistry, pharmacology)
• HIV Infections (drug therapy)
• HIV Integrase (metabolism)
• HIV Integrase Inhibitors (chemistry, pharmacology)
• HIV-1 (drug effects, enzymology)
• Humans