title: Non-thiol farnesyltransferase inhibitors: FTase-inhibition and cellular activity of benzophenone-based bisubstrate analogue farnesyltransferase inhibitors.
abstract: Some 5-acylaminoacylamino-benzophenone derivatives were designed as bisubstrate analogue farnesyltransferase inhibitors. These compounds turned out to be only weakly active against farnesyltransferase, but displayed an antiproliferative effect rendering them suitable for further development as a novel type of cytostatic agents.
authors.affiliation: Institut für Pharmazeutische Chemie, Philipps-Universität Marburg, Marburg, Germany.
authors.forename: Andreas
authors.initials: A
authors.lastname: Mitsch
authors.forename: Silke
authors.initials: S
authors.lastname: Bergemann
authors.forename: Ronald
authors.initials: R
authors.lastname: Gust
authors.forename: Isabel
authors.initials: I
authors.lastname: Sattler
authors.forename: Martin
authors.initials: M
authors.lastname: Schlitzer
mesh_terms: D019883:Alkyl and Aryl Transferases / Q000037:antagonists & inhibitors*; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001577:Benzophenones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002470:Cell Survival / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D051231:Farnesyltranstransferase; D020128:Inhibitory Concentration 50; D013329:Structure-Activity Relationship; D013438:Sulfhydryl Compounds / Q000737:chemistry; D014407:Tumor Cells, Cultured
chemical_list: D000970:Antineoplastic Agents; D001577:Benzophenones; D004791:Enzyme Inhibitors; D013438:Sulfhydryl Compounds; D019883:Alkyl and Aryl Transferases; D051231:Farnesyltranstransferase