title: Quinazolinethiones and quinazolinediones, novel inhibitors of inosine monophosphate dehydrogenase: synthesis and initial structure-activity relationships.
abstract: The development of a series of novel quinazolinethiones and quinazolinediones as inhibitors of inosine monophosphate dehydrogenase (IMPDH) is described. The synthesis, in vitro inhibitory values for IMPDH II and in vitro inhibitory value for PBMC proliferation are discussed.
authors.affiliation: Celltech R and D, Granta Park, Great Abington, Cambridge CB1 6GS, UK.
authors.forename: George M
authors.initials: GM
authors.lastname: Buckley
authors.forename: Natasha
authors.initials: N
authors.lastname: Davies
authors.forename: Hazel J
authors.initials: HJ
authors.lastname: Dyke
authors.forename: Philip J
authors.initials: PJ
authors.lastname: Gilbert
authors.forename: Duncan R
authors.initials: DR
authors.lastname: Hannah
authors.forename: Alan F
authors.initials: AF
authors.lastname: Haughan
authors.forename: Caroline A
authors.initials: CA
authors.lastname: Hunt
authors.forename: William R
authors.initials: WR
authors.lastname: Pitt
authors.forename: Rachael H
authors.initials: RH
authors.lastname: Profit
authors.forename: Nicholas C
authors.initials: NC
authors.lastname: Ray
authors.forename: Marianna D
authors.initials: MD
authors.lastname: Richard
authors.forename: Andrew
authors.initials: A
authors.lastname: Sharpe
authors.forename: Alicia J
authors.initials: AJ
authors.lastname: Taylor
authors.forename: Justine M
authors.initials: JM
authors.lastname: Whitworth
authors.forename: Sophie C
authors.initials: SC
authors.lastname: Williams
mesh_terms: D001773:Blood Cells; D049109:Cell Proliferation / Q000187:drug effects; D004791:Enzyme Inhibitors / Q000138:chemical synthesis; D006801:Humans; D007168:IMP Dehydrogenase / Q000037:antagonists & inhibitors*; D020128:Inhibitory Concentration 50; D007659:Ketones / Q000138:chemical synthesis / Q000494:pharmacology; D009000:Monocytes / Q000187:drug effects; D011799:Quinazolines / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013871:Thiones / Q000138:chemical synthesis / Q000494:pharmacology
chemical_list: D004791:Enzyme Inhibitors; D007659:Ketones; D011799:Quinazolines; D013871:Thiones; D007168:IMP Dehydrogenase; C488211:IMPDH1 protein, human