title: Novel guanidine-based inhibitors of inosine monophosphate dehydrogenase.
abstract: A series of novel guanidine-based small molecule inhibitors of inosine monophosphate dehydrogenase (IMPDH) was explored. IMPDH catalyzes the rate determining step in guanine nucleotide biosynthesis and is a target for anticancer, immunosuppressive and antiviral therapy. The synthesis and the structure-activity relationships (SARs), derived from in vitro studies, for this new series of inhibitors is given.
authors.affiliation: Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543-4000, USA. iwanowie@bms.com
authors.forename: Edwin J
authors.initials: EJ
authors.lastname: Iwanowicz
authors.forename: Scott H
authors.initials: SH
authors.lastname: Watterson
authors.forename: Chunjian
authors.initials: C
authors.lastname: Liu
authors.forename: Henry H
authors.initials: HH
authors.lastname: Gu
authors.forename: Toomas
authors.initials: T
authors.lastname: Mitt
authors.forename: Katerina
authors.initials: K
authors.lastname: Leftheris
authors.forename: Joel C
authors.initials: JC
authors.lastname: Barrish
authors.forename: Catherine A
authors.initials: CA
authors.lastname: Fleener
authors.forename: Katherine
authors.initials: K
authors.lastname: Rouleau
authors.forename: N Z
authors.initials: NZ
authors.lastname: Sherbina
authors.forename: Diane L
authors.initials: DL
authors.lastname: Hollenbaugh
mesh_terms: D000998:Antiviral Agents / Q000138:chemical synthesis / Q000494:pharmacology; D018360:Crystallography, X-Ray; D004305:Dose-Response Relationship, Drug; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D019791:Guanidine / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D007168:IMP Dehydrogenase / Q000037:antagonists & inhibitors*; D007202:Indicators and Reagents; D013329:Structure-Activity Relationship
chemical_list: D000998:Antiviral Agents; D004791:Enzyme Inhibitors; D007202:Indicators and Reagents; D007168:IMP Dehydrogenase; D019791:Guanidine