1186040-65-2Relevant academic research and scientific papers
7-(4H-1,2,4-Triazol-3-yl)benzo[c][2,6]naphthyridines: A novel class of Pim kinase inhibitors with potent cell antiproliferative activity
Pierre, Fabrice,Stefan, Eric,Nédellec, Anne-Sophie,Chevrel, Marie-Claire,Regan, Collin F.,Siddiqui-Jain, Adam,MacAlino, Diwata,Streiner, Nicole,Drygin, Denis,Haddach, Mustapha,O'Brien, Sean E.,Anderes, Kenna,Ryckman, David M.
, p. 6687 - 6692 (2011/12/05)
A novel class of pan-Pim kinase inhibitors was designed by modifying the CK2 inhibitor CX-4945. Introduction of a triazole or secondary amide functionality on the C-7 position and 2′-halogenoanilines on C-5 resulted in potent inhibitors of the Pim-1 and Pim-2 isoforms, with many analogs active at single digit nanomolar concentrations. The molecules inhibited the phosphorylation at Serine 112 of the apoptosis effector BAD, and had potent antiproliferative effects on the AML cell line MV-4-11 (IC50 30 nM). This work delivers an excellent lead-optimization platform for Pim targeting anticancer therapies.
