104877-13-6Relevant articles and documents
Optimization of a pyrazoloquinolinone class of Chk1 kinase inhibitors
Brnardic, Edward J.,Garbaccio, Robert M.,Fraley, Mark E.,Tasber, Edward S.,Steen, Justin T.,Arrington, Kenneth L.,Dudkin, Vadim Y.,Hartman, George D.,Stirdivant, Steven M.,Drakas, Bob A.,Rickert, Keith,Walsh, Eileen S.,Hamilton, Kelly,Buser, Carolyn A.,Hardwick, James,Tao, Weikang,Beck, Stephen C.,Mao, Xianzhi,Lobell, Robert B.,Sepp-Lorenzino, Laura,Yan, Youwei,Ikuta, Mari,Munshi, Sanjeev K.,Kuo, Lawrence C.,Kreatsoulas, Constantine
, p. 5989 - 5994 (2007)
The development of 2,5-dihydro-4H-pyrazolo[4,3-c]quinolin-4-ones as inhibitors of Chk1 kinase is described. Introduction of a fused ring at the C7/C8 positions of the pyrazoloquinolinone provided an increase in potency while guidance from overlapping inhibitor bound Chk1 X-ray crystal structures contributed to the discovery of a potent and solubilizing propyl amine moiety in compound 52 (Chk1 IC50 = 3.1 nM).
INHIBITORS OF CHECKPOINT KINASES
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Page/Page column 32, (2008/06/13)
The instant invention provides for compounds which comprise fused pyrazoles that inhibit CHK1 activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting CHK1 activity by administering the compound
