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. 2007 Jul 1;17(13):3660-5.
doi: 10.1016/j.bmcl.2007.04.045. Epub 2007 Apr 25.

Hit-to-lead studies on benzimidazole inhibitors of ITK: discovery of a novel class of kinase inhibitors

Roger J Snow  1 , Asitha Abeywardane, Scot Campbell, John Lord, Mohammed A Kashem, Hnin Hnin Khine, Josephine King, Jennifer A Kowalski, Steven S Pullen, Teresa Roma, Gregory P Roth, Christopher R Sarko, Noel S Wilson, Michael P Winters, John P Wolak, Charles L Cywin
Affiliations

Hit-to-lead studies on benzimidazole inhibitors of ITK: discovery of a novel class of kinase inhibitors

Roger J Snow et al. Bioorg Med Chem Lett. .

Abstract

Benzimidazole 1 was identified as a selective inhibitor of ITK by high throughput screening. Hit-to-lead studies defined the SAR at all three substituents. Reversing the amide linkage at C6 led to 16, with a fivefold improvement of potency. This enhancement is rationalized by the conformational preference of the substituent. A model for the binding of the benzimidazoles to the ATP-binding site of ITK is proposed.

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