1359754-66-7Relevant academic research and scientific papers
Replacing triazole with diazole to optimize physicochemical properties of a click-based lead compound
Tian, Yinping,Lv, Wenhui,Meng, Qiuyue,Li, Xuewei,Zeng, Wei,Lu, Yaxin,Wang, Peng G.,Jin, Jin,Shen, Jie
, p. 2007 - 2014 (2017/08/03)
This work mainly demonstrated how the physicochemical properties of a click-based lead compound would be affected by the replacement of its triazole ring with a pyrazole or an imidazole ring. Compound A1, a click-based lead from our previous work, was a selective and moderate inhibitor against VEGFR2. Eight new derivatives of A1 were synthesized, from which a pyrazole derivative B2 was selected as a new lead. B2 maintained the in vitro activity of A1. The solubilities of B2 at pH 2.0 and pH 7.4 were enhanced to 1310 and 1.7 μg/mL, respectively. Its log D value of 3.4 would favor B2 to be modified with hydrophilic fragments to further improve intestinal solubility in our future work.
Discovery and structural insight of a highly selective protein kinase inhibitor hit through click chemistry
Gu, Guoxian,Wang, Huihui,Liu, Pi,Fu, Chenzeng,Li, Zhonghua,Cao, Xuefeng,Li, Yunping,Fang, Qinghong,Xu, Feng,Shen, Jie,Wang, Peng George
, p. 2788 - 2790 (2012/04/23)
Novel bisaryl maleimide derivatives to mimic natural kinase inhibitors were prepared through click chemistry. A highly selective hit was discovered in a 124-kinase-assay, and docking studies revealed a π-π stacking interaction with the Phe67 at the P-loop of GSK-3β kinase. The Royal Society of Chemistry 2012.
