title: 2-(Arylpropionylamino)- and 2-(arylacryloylamino)benzophenones: farnesyltransferase inhibition and antimalarial activity.
abstract: Structural variation of the 2-acylamino moiety of some benzophenone farnesyltransferase inhibitors led to the para-trifluoromethylphenylpropionyl derivative with relatively low farnesyltransferase inhibition but considerable antimalarial activity and no cytotoxicity.
authors.affiliation: Department für Pharmazie, Zentrum für Pharmaforschung, Ludwig-Maximilians-Universität München, Germany.
authors.forename: K
authors.initials: K
authors.lastname: Fucik
authors.forename: K
authors.initials: K
authors.lastname: Kettler
authors.forename: J
authors.initials: J
authors.lastname: Wiesner
authors.forename: R
authors.initials: R
authors.lastname: Ortmann
authors.forename: D
authors.initials: D
authors.lastname: Unterreitmeier
authors.forename: J
authors.initials: J
authors.lastname: Krauss
authors.forename: F
authors.initials: F
authors.lastname: Bracher
authors.forename: H
authors.initials: H
authors.lastname: Jomaa
authors.forename: M
authors.initials: M
authors.lastname: Schlitzer
mesh_terms: D019883:Alkyl and Aryl Transferases / Q000037:antagonists & inhibitors*; D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000494:pharmacology*; D001577:Benzophenones / Q000138:chemical synthesis* / Q000494:pharmacology*; D004354:Drug Screening Assays, Antitumor; D004926:Escherichia coli / Q000187:drug effects / Q000201:enzymology; D051231:Farnesyltranstransferase; D018922:HL-60 Cells; D006801:Humans; D007202:Indicators and Reagents; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D010963:Plasmodium falciparum / Q000187:drug effects; D013050:Spectrometry, Fluorescence; D013329:Structure-Activity Relationship; D013778:Tetrazolium Salts; D013844:Thiazoles
chemical_list: D000962:Antimalarials; D001577:Benzophenones; D007202:Indicators and Reagents; D013778:Tetrazolium Salts; D013844:Thiazoles; D019883:Alkyl and Aryl Transferases; D051231:Farnesyltranstransferase; C022616:thiazolyl blue