872510-82-2Relevant articles and documents
Discovery of novel Bcr-Abl inhibitors targeting myristoyl pocket and ATP site
Dong, Jinyun,Lu, Wen,Pan, Xiaoyan,Su, Ping,Shi, Yaling,Wang, Jinfeng,Zhang, Jie
, p. 6876 - 6884 (2015/01/09)
Bcr-Abl plays an essential role in the pathogenesis and development of chronic myeloid leukaemia (CML). Inhibition of Bcr-Abl has great potential for therapeutic intervention in CML. In order to obtain novel and potent Bcr-Abl inhibitors, twenty seven 4,6-disubstituted pyrimidines were synthesized and evaluated herein. The biological results indicated that four compounds of them (C4, C5, C16, and C23) were potent Bcr-Abl inhibitors which were comparable to positive control. Moreover, C4 and C5 displayed promising antiproliferative activity against K562 cells. The results suggested that these 4,6-disubstituted pyrimidines could serve as promising leads for further optimization of Bcr-Abl inhibitors.
COMPOUNDS AND COMPOSITIONS FOR PROTEIN KINASE INHBITORS
-
Page/Page column 21-22, (2008/06/13)
The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly di
Discovery of EGFR selective 4,6-disubstituted pyrimidines from a combinatorial kinase-directed heterocycle library
Zhang, Qiong,Liu, Yi,Gao, Feng,Ding, Qiang,Cho, Charles,Hur, Wooyoung,Jin, Yunho,Uno, Tetsuo,Joazeiro, Claudio A. P.,Gray, Nathanael
, p. 2182 - 2183 (2007/10/03)
The epidermal growth factor receptor (EGFR) tyrosine kinase was one of the first receptor tyrosine kinases to be targeted for drug development by the pharmaceutical industry due to its ubiquitous overexpression in a variety of tumors. Despite the validati
PYRIMIDINE UREA DERIVATIVES AS KINASE INHIBITORS
-
Page/Page column 193-194, (2008/06/13)
The invention relates to compounds of formula (I) wherein the substituents X1, R1, R2, R3 and R4 have the meaning as set forth and explained in the description of the invention, to processes for the preparation of these compounds, pharmaceutical compositions containing same, the use thereof optionally in combination with one or more other pharmaceutically active compounds for the therapy of a disease which responds to an inhibition of protein kinase activity, and a method for the treatment of such a disease.