title: Structure-activity relationships of novel anti-malarial agents part 8. Effect of different central aryls in biarylacryloylaminobenzophenones on antimalarial activity.
abstract: Replacement of the 2,5-disubstituted furyl residue present in the known antimalarial agents 8 by other aryl residues resulted in a more or less reduced antimalarial activity in most cases. The only exemption was the 2,4-thienylene compound 11a displaying activity with an IC50 value of 120 nM. In conclusion, the 2,5-furylene compound 8e remains to represent the most active antimalarial agent in this series of farnesyltransferase inhibitors.
authors.affiliation: Biochemisches Institut der Justus-Liebig-Universität Giessen, Germany.
authors.forename: J
authors.initials: J
authors.lastname: Wiesner
authors.forename: A
authors.initials: A
authors.lastname: Mitsch
authors.forename: M
authors.initials: M
authors.lastname: Altenkämper
authors.forename: R
authors.initials: R
authors.lastname: Ortmann
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 / Q000737:chemistry* / Q000494:pharmacology*; D001577:Benzophenones / Q000737:chemistry* / Q000494:pharmacology*; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D051231:Farnesyltranstransferase; D007202:Indicators and Reagents; D008968:Molecular Conformation; D010963:Plasmodium falciparum / Q000187:drug effects / Q000254:growth & development; D013329:Structure-Activity Relationship
chemical_list: D000962:Antimalarials; D001577:Benzophenones; D004791:Enzyme Inhibitors; D007202:Indicators and Reagents; D019883:Alkyl and Aryl Transferases; D051231:Farnesyltranstransferase