658700-02-8Relevant articles and documents
Hit-to-lead studies on benzimidazole inhibitors of ITK: Discovery of a novel class of kinase inhibitors
Snow, Roger J.,Abeywardane, Asitha,Campbell, Scot,Lord, John,Kashem, Mohammed A.,Khine, Hnin Hnin,King, Josephine,Kowalski, Jennifer A.,Pullen, Steven S.,Roma, Teresa,Roth, Gregory P.,Sarko, Christopher R.,Wilson, Noel S.,Winters, Michael P.,Wolak, John P.,Cywin, Charles L.
, p. 3660 - 3665 (2008/02/09)
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 enhanceme
