Vibha Oza 1 , Susan Ashwell , Patrick Brassil , Jason Breed , Chun Deng , Jay Ezhuthachan , Heather Haye , Candice Horn , James Janetka , Paul Lyne , Nicholas Newcombe , Ludo Otterbien , Martin Pass , Jon Read , Sian Roswell , Mei Su , Dorin Toader , Dingwei Yu , Yan Yu , Anna Valentine , Peter Webborn , Ann White , Sonya Zabludoff , Xiaolan Zheng
Sep 01 2010
Checkpoint Kinase-1 (Chk1, CHK1, CHEK1) is a Ser/Thr protein kinase that mediates cellular responses to DNA-damage. A novel class of Chk1 inhibitors, triazoloquinolones/triazolones (TZ's) was identified by high throughput screening. The optimization of these hits to provide a lead series is described.