Title of article :
Investigation of novel 7,8-disubstituted-5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-ones as potent Chk1 inhibitors
Author/Authors :
Lisa A. Hasvold، نويسنده , , L.E. Wang، نويسنده , , Magdalena Przytulinska، نويسنده , , Zhan Xiao، نويسنده , , Zehan Chen، نويسنده , , Wen-Zhen Gu، نويسنده , , Philip J. Merta، نويسنده , , John Xue، نويسنده , , Peter Kovar، نويسنده , , Haiying Zhang، نويسنده , , Chang Park، نويسنده , , Thomas J. Sowin، نويسنده , , Saul H. Rosenberg، نويسنده , , Nan-Horng Lin، نويسنده ,
Abstract :
The synthesis and structure–activity relationships (SAR) of Chk1 inhibitors based on a 5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-one core are described. Specifically, an exploration of the 7 and 8 positions on this previously disclosed core afforded compounds with improved enzymatic and cellular potency.
