title: Novel indole-based inhibitors of IMPDH: introduction of hydrogen bond acceptors at indole C-3.
abstract: The development of a series of novel indole-based inhibitors of 5'-inosine monophosphate dehydrogenase (IMPDH) is described. Various hydrogen bond acceptors at C-3 of the indole were explored. The synthesis and the structure-activity relationships (SARs) derived from in vitro studies are outlined.
authors.affiliation: Bristol-Myers Squibb PRI, Princeton, NJ 08543-4000, USA. scott.watterson@bms.com
authors.forename: Scott H
authors.initials: SH
authors.lastname: Watterson
authors.forename: T G Murali
authors.initials: TG
authors.lastname: Dhar
authors.forename: Shelley K
authors.initials: SK
authors.lastname: Ballentine
authors.forename: Zhongqi
authors.initials: Z
authors.lastname: Shen
authors.forename: Joel C
authors.initials: JC
authors.lastname: Barrish
authors.forename: Daniel
authors.initials: D
authors.lastname: Cheney
authors.forename: Catherine A
authors.initials: CA
authors.lastname: Fleener
authors.forename: Katherine A
authors.initials: KA
authors.lastname: Rouleau
authors.forename: Robert
authors.initials: R
authors.lastname: Townsend
authors.forename: Diane L
authors.initials: DL
authors.lastname: Hollenbaugh
authors.forename: Edwin J
authors.initials: EJ
authors.lastname: Iwanowicz
mesh_terms: D002455:Cell Division / Q000187:drug effects; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D020719:Glucuronides / Q000378:metabolism; D006801:Humans; D006860:Hydrogen Bonding; D007168:IMP Dehydrogenase / Q000037:antagonists & inhibitors*; D007107:Immune System / Q000187:drug effects; D007211:Indoles / Q000737:chemistry*; D007527:Isoenzymes / Q000037:antagonists & inhibitors; D008934:Mitogens / Q000494:pharmacology; D015363:Quinolones / Q000138:chemical synthesis / Q000494:pharmacology; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D004791:Enzyme Inhibitors; D020719:Glucuronides; D007211:Indoles; D007527:Isoenzymes; D008934:Mitogens; D015363:Quinolones; D007168:IMP Dehydrogenase