370866-02-7Relevant articles and documents
Identification of inhibitors of checkpoint kinase 1 through template screening
Matthews, Thomas P.,Klair, Suki,Burns, Samantha,Boxall, Kathy,Cherry, Michael,Fisher, Martin,Westwood, Isaac M.,Walton, Michael I.,McHardy, Tatiana,Cheung, Kwai-Ming J.,Van Montfort, Rob,Williams, David,Aherne, G. Wynne,Garrett, Michelle D.,Reader, John,Collins, Ian
experimental part, p. 4810 - 4819 (2010/03/01)
Checkpoint kinase 1 (CHK1) is an oncology target of significant current interest. Inhibition of CHK1 abrogates DNA damage-induced cell cycle checkpoints and sensitizes p53 deficient cancer cells to genotoxic therapies. Using template screening, a fragment
1H-pyrazolo[3,4-b]pyridine inhibitors of cyclin-dependent kinases: Highly potent 2,6-difluorophenacyl analogues
Misra, Raj N.,Xiao, Hai-Yun,Rawlins, David B.,Shan, Weifang,Kellar, Kristen A.,Mulheron, Janet G.,Sack, John S.,Tokarski, John S.,Kimball, S. David,Webster, Kevin R.
, p. 2405 - 2408 (2007/10/03)
Structure-activity studies of 1H-pyrazolo[3,4-b]pyridine 1 have resulted in the discovery of potent CDK1/CDK2 selective inhibitor 21h, BMS-265246 (CDK1/cycB IC50=6 nM, CDK2/cycE IC50=9 nM). The 2,6-difluorophenyl substitution was cri