Zhu, Heping; Ying, Shilong; Zhou, Bingluo; Liang, Xiao; He, Quan; Song, Ping; Hu, Xinyang; Shi, Keqiang; Xiong, Mingteng; Jin, Hongchuan; Pan, Yuanjiang published an article on February 5 ,2021. The article was titled 《Discovery of novel 2-aryl-3-sulfonamido-pyridines (HoAns) as microtubule polymerization inhibitors with potent antitumor activities》, and you may find the article in European Journal of Medicinal Chemistry.Application In Synthesis of 2-Bromopyridin-3-amine The information in the text is summarized as follows:
In this study, a series of novel 2-aryl-3-sulfonamido-pyridines had been designed, synthesized, and evaluated for their antiproliferative activities in vitro and in vivo. Among them, compound I exhibited the most potent activity with IC50 values ranging from 0.170 to 1.193μM in a panel of cancer cell lines. Mechanistic studies indicated that compound I bound to the colchicine site of β-tubulin, resulting in colony formation inhibition, G2/M phase cell cycle arrest, cell apoptosis as well as increased the generation of ROS in both RKO and SW620 cells. In addition, compound I showed potent anti-vascular activity in vitro. Furthermore, compound I also exhibited outstanding antitumor activity in SW620 xenograft tumor models without observable toxic effects, which was more potent than that of ABT-751. In conclusion, these findings suggest that compound I may be a promising microtubule destabilizing agent and deserves for further development in cancer therapy. The experimental process involved the reaction of 2-Bromopyridin-3-amine(cas: 39856-58-1Application In Synthesis of 2-Bromopyridin-3-amine)
2-Bromopyridin-3-amine(cas: 39856-58-1) belongs to anime. Amines have a free lone pair with which they can coordinate to metal centers. Amine–metal bonds are weaker because amines are incapable of backbonding, but they are still important for sensing applications.While stronger than hydrogen bonds, amine–metal bonds are still weaker than both covalent and ionic bonds.Application In Synthesis of 2-Bromopyridin-3-amine