Title of article :
The development of novel 1,2-dihydro-pyrimido[4,5-c]pyridazine based inhibitors of lymphocyte specific kinase (Lck)
Author/Authors :
Mark Sabat، نويسنده , , John C. VanRens، نويسنده , , Todd A. Brugel، نويسنده , , Jennifer Maier، نويسنده , , Matthew J. Laufersweiler، نويسنده , , Adam Golebiowski، نويسنده , , Biswanath De، نويسنده , , Vijayasurian Easwaran، نويسنده , , Lily C. Hsieh، نويسنده , , Jeff Rosegen، نويسنده , , Steve Berberich، نويسنده , , Eric Suchanek، نويسنده , , Michael J. Janusz، نويسنده ,
Abstract :
This communication details the synthesis, biological activity, and proposed binding mode of a novel class of tri-cyclic derivatives of 1,2-dihydro-pyrimido[4,5-c]pyridazines 1 and 2. The most potent analogs disclosed showed low nanomolar activity for the inhibition of Lck kinase.
Keywords :
T-cell , Lymphocyte specific kinase , Lck , pyridazines
