title: Novel lead structures for antimalarial farnesyltransferase inhibitors.
abstract: Through the combination of nitrophenylfurylacryloyl moiety which has been designed to occupy an aryl binding site of farnesyltransferase with several AA(X)-peptidomimetic substructures some novel farnesyltransferase inhibitors were obtained. Evaluation of their antimalarial activity and some initial modifications yielded a 4-benzophenone- and a sulfonamid-based novel lead for antimalarial farnesyltransferase inhibitors.
authors.affiliation: Department für Pharmazie, Zentrum für Pharmaforschung, Ludwig-Maximilians-Universität München, Germany.
authors.forename: K
authors.initials: K
authors.lastname: Kettler
authors.forename: J
authors.initials: J
authors.lastname: Sakowski
authors.forename: J
authors.initials: J
authors.lastname: Wiesner
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* / Q000096:biosynthesis; D000588:Amines / Q000138:chemical synthesis / Q000494:pharmacology; D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000494:pharmacology; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D051231:Farnesyltranstransferase; D009682:Magnetic Resonance Spectroscopy; D009574:Nitro Compounds / Q000138:chemical synthesis / Q000494:pharmacology; D010963:Plasmodium falciparum / Q000187:drug effects / Q000201:enzymology / Q000254:growth & development; D012441:Saccharomyces cerevisiae / Q000201:enzymology
chemical_list: D000588:Amines; D000962:Antimalarials; D004791:Enzyme Inhibitors; D009574:Nitro Compounds; D019883:Alkyl and Aryl Transferases; D051231:Farnesyltranstransferase