title: 2-Aryl benzimidazoles featuring alkyl-linked pendant alcohols and amines as inhibitors of checkpoint kinase Chk2.
abstract: A series of benzimidazole compounds containing pendant alcohol and amine moieties was found to be active against checkpoint kinase Chk2. These compounds were prepared to examine a potential hydrogen bond interaction with an active site residue and to investigate replacement of a biaryl linker with an aliphatic system in an effort to improve solubility.
authors.affiliation: Johnson & Johnson Pharmaceutical Research & Development, L.L.C, 3210 Merryfield Row, San Diego, CA 92121, USA. dneff1@prdus.jnj.com
authors.forename: Danielle K
authors.initials: DK
authors.lastname: Neff
authors.forename: Alice
authors.initials: A
authors.lastname: Lee-Dutra
authors.forename: Jonathan M
authors.initials: JM
authors.lastname: Blevitt
authors.forename: Frank U
authors.initials: FU
authors.lastname: Axe
authors.forename: Michael D
authors.initials: MD
authors.lastname: Hack
authors.forename: Johnathan C
authors.initials: JC
authors.lastname: Buma
authors.forename: Raymond
authors.initials: R
authors.lastname: Rynberg
authors.forename: Anders
authors.initials: A
authors.lastname: Brunmark
authors.forename: Lars
authors.initials: L
authors.lastname: Karlsson
authors.forename: J Guy
authors.initials: JG
authors.lastname: Breitenbucher
mesh_terms: D000438:Alcohols / Q000737:chemistry* / Q000494:pharmacology; D000588:Amines / Q000737:chemistry* / Q000494:pharmacology; D001562:Benzimidazoles / Q000737:chemistry* / Q000494:pharmacology; D064447:Checkpoint Kinase 2; D006860:Hydrogen Bonding; D047428:Protein Kinase Inhibitors / Q000737:chemistry* / Q000494:pharmacology; D017346:Protein Serine-Threonine Kinases / Q000037:antagonists & inhibitors*
chemical_list: D000438:Alcohols; D000588:Amines; D001562:Benzimidazoles; D047428:Protein Kinase Inhibitors; D064447:Checkpoint Kinase 2; D017346:Protein Serine-Threonine Kinases