2-(Arylpropionylamino)- and 2-(arylacryloylamino)benzophenones: farnesyltransferase inhibition and antimalarial activity.
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.
Fucik
K
K
Department für Pharmazie, Zentrum für Pharmaforschung, Ludwig-Maximilians-Universität München, Germany.
Kettler
K
K
Wiesner
J
J
Ortmann
R
R
Unterreitmeier
D
D
Krauss
J
J
Bracher
F
F
Jomaa
H
H
Schlitzer
M
M
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
D000962:Antimalarials; D001577:Benzophenones; D007202:Indicators and Reagents; D013778:Tetrazolium Salts; D013844:Thiazoles; D019883:Alkyl and Aryl Transferases; D051231:Farnesyltranstransferase; C022616:thiazolyl blue