title: Novel non-benzimidazole chk2 kinase inhibitors.
abstract: In a recent paper, [Arienti, K. L.; Brunmark, A.; Axe, F. U.; McClure, K. M.; Lee, A.; Blevitt, J.; Neff, D. K.; Huang, L.; Crawford, S.; Chennagiri, R. P.; Karlsson, L.; Brietenbucher, J. G. J. Med. Chem.2005, 48, 1873], we described the discovery of a class of benzimidazole chk2 kinase inhibitors, exemplified by compound 1, which had radio-protective effects in human T-cells subjected to ionizing radiation. Here, a series of non-benzimidazole analogs intended to define the scope of the SAR about this new series of inhibitor, and allow for refinement of the binding model of these compounds to the chk2 kinase is described.
authors.affiliation: Johnson and Johnson Pharmaceutical Research and Development, LLC, 3210 Merryfield Row, San Diego, CA 92121, USA. kmcclure@prdus.jnj.com
authors.forename: Kelly J
authors.initials: KJ
authors.lastname: McClure
authors.forename: Liming
authors.initials: L
authors.lastname: Huang
authors.forename: Kristen L
authors.initials: KL
authors.lastname: Arienti
authors.forename: Frank U
authors.initials: FU
authors.lastname: Axe
authors.forename: Anders
authors.initials: A
authors.lastname: Brunmark
authors.forename: Jon
authors.initials: J
authors.lastname: Blevitt
authors.forename: J Guy
authors.initials: JG
authors.lastname: Breitenbucher
mesh_terms: D001562:Benzimidazoles / Q000737:chemistry / Q000494:pharmacology; D064447:Checkpoint Kinase 2; D008958:Models, Molecular; D047428:Protein Kinase Inhibitors / Q000737:chemistry* / Q000494:pharmacology; D017346:Protein Serine-Threonine Kinases / Q000037:antagonists & inhibitors*; D011837:Radiation-Protective Agents / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D001562:Benzimidazoles; D047428:Protein Kinase Inhibitors; D011837:Radiation-Protective Agents; D064447:Checkpoint Kinase 2; C578634:CHEK2 protein, human; D017346:Protein Serine-Threonine Kinases