G2 CHECKPOINT INHIBITORS AND ASSAY

摘要

Compounds are provided that inhibit the G2 checkpoint in the cell cycle and are useful for sensitizing G1 deficient cancer cells to killing by DNA damaging agents. Also provided is an assay for G2 checkpoint inhibitors which includes applying a DNA damaging agent to p53 deficient cells and determining whether such cells do not arrest at G2 and proceed to mitosis after application of a sample to be tested. The assay may employ mitotic cell specific monoclonal antibodies. Compounds of this invention have the general formula: <IMG> wherein R5 is selected from the group comprising: <IMG> <IMG> <IMG>