Bioorganic & Medicinal Chemistry Letters 2006-04-01

Novel non-benzimidazole chk2 kinase inhibitors.

Kelly J McClure, Liming Huang, Kristen L Arienti, Frank U Axe, Anders Brunmark, Jon Blevitt, J Guy Breitenbucher

Index: Bioorg. Med. Chem. Lett. 16(7) , 1924-8, (2006)

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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.