1018563-63-7Relevant academic research and scientific papers
Design, synthesis and biological evaluation of novel acrylamide analogues as inhibitors of BCR-ABL kinase
Li, Shuxin,Yao, Zhenglin,Zhao, Yanjin,Chen, Wei,Wang, Huijia,Kuang, Xianzhao,Zhan, Wenhu,Yao, Shan,Yu, Shanyou,Hu, Wenxiang
, p. 5279 - 5282 (2012/09/07)
A series of acrylamide analogues were designed and synthesized from Imatinib and Nilotinib as novel BCR-ABL inhibitors by application of the principle of nonclassical electronic isostere. All new compounds were evaluated for their inhibitory effects on the activity of BCR-ABL kinase and the proliferation of K562 leukemia cancer cells in vitro. The acrylamide analogues in which the substituent in C ring was trifluoromethyl group were identified as highly potent BCR-ABL kinase inhibitors. Compound 13f exhibited an IC 50 value as low as 20.6 nM in ABL kinase inhibition and an IC 50 value of 32.3 nM for antiproliferative activity, about 10.5-fold and 12-fold lower than those of Imatinib respectively. These results suggest that compound 13f is a promising candidate as a novel BCR-ABL kinase inhibitor for further development.
Acrylamide Derivative And Use Thereof In Manufacture Of Medicament
-
Page/Page column 17, (2012/05/20)
An acrylamide derivative represented by formula (I), pharmaceutically acceptable salts and solvates thereof, as well as a medicament containing said acrylamide derivative or its pharmaceutically acceptable salts as the active ingredient, which can be used to treat disorders associated with tyrosine kinase especially Bcr-Abl, including proliferative disorders such as cancers, and inflammation and the like are provided.
