title: Investigation of novel 7,8-disubstituted-5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-ones as potent Chk1 inhibitors.
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.
authors: Abbott Laboratories, Cancer Research, 100 Abbott Park Road, Dept. R4N6 AP10-307, Abbott Park, IL 60064-6101, USA. lisa.hasvold@abbott.com
authors: Lisa A
authors: LA
authors: Hasvold
authors: Le
authors: L
authors: Wang
authors: Magdalena
authors: M
authors: Przytulinska
authors: Zhan
authors: Z
authors: Xiao
authors: Zehan
authors: Z
authors: Chen
authors: Wen-Zhen
authors: WZ
authors: Gu
authors: Philip J
authors: PJ
authors: Merta
authors: John
authors: J
authors: Xue
authors: Peter
authors: P
authors: Kovar
authors: Haiying
authors: H
authors: Zhang
authors: Chang
authors: C
authors: Park
authors: Thomas J
authors: TJ
authors: Sowin
authors: Saul H
authors: SH
authors: Rosenberg
authors: Nan-Horng
authors: NH
authors: Lin
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D001570:Benzodiazepinones / Q000138:chemical synthesis / Q000494:pharmacology*; D045744:Cell Line, Tumor / Q000187:drug effects; D000071877:Checkpoint Kinase 1; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology*; D006367:HeLa Cells; D006801:Humans; D008956:Models, Chemical; D011485:Protein Binding; D011494:Protein Kinases / Q000378:metabolism*; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D001570:Benzodiazepinones; D004791:Enzyme Inhibitors; D011494:Protein Kinases; C000605867:CHEK1 protein, human; D000071877:Checkpoint Kinase 1