889939-25-7Relevant articles and documents
The condensed heterocyclic compound such as Bruton kinase inhibitors (by machine translation)
-
Paragraph 0190-0193, (2018/04/20)
The invention relates to a fused heterocycle derivative and an application, which has a structure shown in a formula 1). The compound with the structure shown in the formula 1) has good inhibition effect to Bruton kinases activity, and median inhibitory concentration is lower than 10mol.L generally.
New thiazole carboxamides as potent inhibitors of Akt kinases
Chang, Shaohua,Zhang, Zhang,Zhuang, Xiaoxi,Luo, Jinfeng,Cao, Xianwen,Li, Honglin,Tu, Zhengchao,Lu, Xiaoyun,Ren, Xiaomei,Ding, Ke
, p. 1208 - 1212 (2012/03/11)
A new series of 2-substituted thiazole carboxamides were identified as potent pan inhibitors against all three isoforms of Akt (Akt1, Akt2 and Akt3) by systematic optimization of weak screening hit N-(1-amino-3-phenylpropan-2-yl)- 2-phenylthiazole-5-carboxamide (1). One of the most potent compounds, 5m, inhibited the kinase activities of Akt1, Akt2 and Akt3 with IC50 values of 25, 196 and 24 nM, respectively. The compound also potently inhibited the phosphorylation of downstream MDM2 and GSK3β proteins, and displayed strongly antiproliferative activity in prostate cancer cells. The inhibitors might serve as lead compounds for further development of novel effective anticancer agents.