2-Aryl benzimidazoles featuring alkyl-linked pendant alcohols and amines as inhibitors of checkpoint kinase Chk2

Danielle K Neff; Alice Lee-Dutra; Jonathan M Blevitt; Frank U Axe; Michael D Hack; Johnathan C Buma; Raymond Rynberg; Anders Brunmark; Lars Karlsson; J Guy Breitenbucher

doi:10.1016/j.bmcl.2007.09.098

2-Aryl benzimidazoles featuring alkyl-linked pendant alcohols and amines as inhibitors of checkpoint kinase Chk2

Bioorg Med Chem Lett. 2007 Dec 1;17(23):6467-71. doi: 10.1016/j.bmcl.2007.09.098. Epub 2007 Oct 4.

Authors

Danielle K Neff¹, Alice Lee-Dutra, Jonathan M Blevitt, Frank U Axe, Michael D Hack, Johnathan C Buma, Raymond Rynberg, Anders Brunmark, Lars Karlsson, J Guy Breitenbucher

Affiliation

¹ Johnson & Johnson Pharmaceutical Research & Development, L.L.C, 3210 Merryfield Row, San Diego, CA 92121, USA. dneff1@prdus.jnj.com

PMID: 17937984
DOI: 10.1016/j.bmcl.2007.09.098

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.

Publication types

Comparative Study

MeSH terms

Alcohols / chemistry*
Alcohols / pharmacology
Amines / chemistry*
Amines / pharmacology
Benzimidazoles / chemistry*
Benzimidazoles / pharmacology
Checkpoint Kinase 2
Hydrogen Bonding
Protein Kinase Inhibitors / chemistry*
Protein Kinase Inhibitors / pharmacology
Protein Serine-Threonine Kinases / antagonists & inhibitors*

Substances

Alcohols
Amines
Benzimidazoles
Protein Kinase Inhibitors
Checkpoint Kinase 2
Protein Serine-Threonine Kinases