2-Aryl benzimidazoles featuring alkyl-linked pendant alcohols and amines as inhibitors of checkpoint kinase Chk2.
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.
Neff
Danielle K
DK
Johnson & Johnson Pharmaceutical Research & Development, L.L.C, 3210 Merryfield Row, San Diego, CA 92121, USA. dneff1@prdus.jnj.com
Lee-Dutra
Alice
A
Blevitt
Jonathan M
JM
Axe
Frank U
FU
Hack
Michael D
MD
Buma
Johnathan C
JC
Rynberg
Raymond
R
Brunmark
Anders
A
Karlsson
Lars
L
Breitenbucher
J Guy
JG
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*
D000438:Alcohols; D000588:Amines; D001562:Benzimidazoles; D047428:Protein Kinase Inhibitors; D064447:Checkpoint Kinase 2; D017346:Protein Serine-Threonine Kinases