title: 2-(aminoacylamino)benzophenones: farnesyltransferase inhibition and antimalarial activity.
abstract: The use of amino acids as acyl substitutents at the 2-amino group of our benzophenone core structure yielded compounds with mainly good to moderate farnesyltransferase inhibitory and moderate antimalarial activity. However, these farnesyltransferase inhibitors display some degree of selectivity towards malarial parasites since there was no cytotoxic activity observed at 70-80 microM.
authors.affiliation: Department für Pharmazie, Zentrum für Pharmaforschung, Ludwig-Maximilians-Universität, München.
authors.forename: K
authors.initials: K
authors.lastname: Kettler
authors.forename: J
authors.initials: J
authors.lastname: Wiesner
authors.forename: K
authors.initials: K
authors.lastname: Fucik
authors.forename: J
authors.initials: J
authors.lastname: Sakowski
authors.forename: R
authors.initials: R
authors.lastname: Ortmann
authors.forename: H M
authors.initials: HM
authors.lastname: Dahse
authors.forename: H
authors.initials: H
authors.lastname: Jomaa
authors.forename: M
authors.initials: M
authors.lastname: Schlitzer
mesh_terms: D000596:Amino Acids / Q000737:chemistry; D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000494:pharmacology*; D001577:Benzophenones / Q000138:chemical synthesis* / Q000494:pharmacology*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D004912:Erythrocytes / Q000469:parasitology; D004926:Escherichia coli / Q000187:drug effects / Q000201:enzymology; D006367:HeLa Cells; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D010963:Plasmodium falciparum / Q000187:drug effects / Q000254:growth & development; D013329:Structure-Activity Relationship
chemical_list: D000596:Amino Acids; D000962:Antimalarials; D001577:Benzophenones; D004791:Enzyme Inhibitors