title: In vitro inhibitory properties of ferrocene-substituted chalcones and aurones on bacterial and human cell cultures.
abstract: Two series of ten chalcones and ten aurones, where ferrocene replaces the C ring and with diverse substituents on the A ring were synthesized. The compounds were tested against two antibiotic-sensitive bacterial strains, E. coli ATCC 25922 and S. aureus ATCC 25923, and two antibiotic-resistant strains, S. aureus SA-1199B and S. epidermidis IPF896. The unsubstituted compound and those with methoxy substitution showed an inhibitory effect on all bacterial strains at minimum inhibitory concentrations ranging between 2 and 32 mg L(-1). For four of these compounds, the effect was bactericidal, as opposed to bacteriostatic. The corresponding organic aurones did not show growth inhibition, underscoring the role of the ferrocene group. The methoxy-substituted aurones and the unsubstituted aurone also showed low micromolar (IC(50)) activity against MRC-5 non-tumoral lung cells and MDA-MB-231 breast cancer cells, suggesting non-specific toxicity.
authors.affiliation: ENSCP Chimie ParisTech, Laboratoire Charles Friedel (LCF), Paris, France.
authors.forename: Keshri Nath
authors.initials: KN
authors.lastname: Tiwari
authors.forename: Jean-Philippe
authors.initials: JP
authors.lastname: Monserrat
authors.forename: Arnaud
authors.initials: A
authors.lastname: Hequet
authors.forename: Carine
authors.initials: C
authors.lastname: Ganem-Elbaz
authors.forename: Thierry
authors.initials: T
authors.lastname: Cresteil
authors.forename: Gérard
authors.initials: G
authors.lastname: Jaouen
authors.forename: Anne
authors.initials: A
authors.lastname: Vessières
authors.forename: Elizabeth A
authors.initials: EA
authors.lastname: Hillard
authors.forename: Claude
authors.initials: C
authors.lastname: Jolivalt
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology / Q000633:toxicity; D001419:Bacteria / Q000187:drug effects*; D001572:Benzofurans / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology* / Q000633:toxicity; D045744:Cell Line, Tumor; D002599:Chalcone / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology* / Q000633:toxicity; D023381:Endpoint Determination; D005296:Ferrous Compounds / Q000737:chemistry*; D006801:Humans; D000075163:Metallocenes; D008826:Microbial Sensitivity Tests; D013997:Time Factors
chemical_list: D000900:Anti-Bacterial Agents; D001572:Benzofurans; D005296:Ferrous Compounds; D000075163:Metallocenes; C486837:aurone; D002599:Chalcone; C004998:ferrocene