《Design, synthesis, and biological evaluation of triazole-based heteroaromatic derivatives as Bcr-Abl kinase inhibitors》 was written by Pan, Xiaoyan; Liu, Nanxin; Liu, Yuying; Zhang, Qingqing; Wang, Kai; Liu, Xueying; Zhang, Jie. Application of 13534-97-9This research focused ontriazole heterocycle preparation kinase inhibitor antitumor apoptosis docking safety; Antileukemic activity; Aromatic heterocycles; Bcr-Abl kinases; In silico modeling study; Proline; Structure-activity relationship; Trizole. The article conveys some information:
A series of compounds with heteroaromatics-triazole scaffold as hinge binding moiety (HBM) were developed as Bcr-Abl inhibitors based on in silico modeling anal. Biol. results indicated that these compounds exhibited a significantly enhanced inhibition against Bcr-Abl WT and Bcr-Abl T315I in kinases assays, along with improved anti-proliferative activities in leukemia cell assays, compared with previous disclosed compounds Meanwhile, the inhibition of Bcr-Abl activity in Ba/F3 cells demonstrated that these compounds exerted effects mainly by acting on Bcr-Abl. Addnl., few compounds effectively induced apoptosis, arrested the cell cycle at S or G2/M phase, and inhibited phosphorylation of Bcr-Abl and STAT5 in a dose-dependent manner. Docking studies indicated that triazole indeed retained the hydrophobic interaction of aromatic heterocycles with hinge region, and ADME prediction suggested that tested compounds had a favorable safety profile. Therefore, aromatic heterocycles incorporated with triazole could serve as a promising HBM for Bcr-Abl inhibitors with proline as flexible linker.6-Bromopyridin-3-amine(cas: 13534-97-9Application of 13534-97-9) was used in this study.
6-Bromopyridin-3-amine(cas: 13534-97-9) belongs to anime. The reaction of alkyl halides, R―X, where X is a halogen, or analogous reagents with ammonia (or amines) is useful with certain compounds. Not all alkyl halides are effective reagents; the reaction is sluggish with secondary alkyl groups and fails with tertiary ones. Its usefulness is largely confined to primary alkyl halides (those having two hydrogen atoms on the reacting site).Application of 13534-97-9