title: 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: ENSCP Chimie ParisTech, Laboratoire Charles Friedel, 75005 Paris, France.
authors: Jean-Philippe
authors: JP
authors: Monserrat
authors: Rasha I
authors: RI
authors: Al-Safi
authors: Keshri Nath
authors: KN
authors: Tiwari
authors: Lionel
authors: L
authors: Quentin
authors: Guy G
authors: GG
authors: Chabot
authors: Anne
authors: A
authors: Vessières
authors: Gérard
authors: G
authors: Jaouen
authors: Nouri
authors: N
authors: Neamati
authors: Elizabeth A
authors: EA
authors: Hillard
mesh_terms: D001881:Borates / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D002599:Chalcone; D047188:Chalcones / Q000737:chemistry* / Q000494:pharmacology*; D015658:HIV Infections / Q000188:drug therapy*; D019427:HIV Integrase / Q000378:metabolism*; D019428:HIV Integrase Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D015497:HIV-1 / Q000187:drug effects* / Q000201:enzymology; D006801:Humans
chemical_list: D001881:Borates; D047188:Chalcones; D019428:HIV Integrase Inhibitors; D002599:Chalcone; D019427:HIV Integrase; C514801:p31 integrase protein, Human immunodeficiency virus 1