202824-49-5Relevant academic research and scientific papers
5-Methoxyquinoline derivatives as a new class of EZH2 inhibitors
Xiang, Pu,Jie, Hui,Zhou, Yang,Yang, Bo,Wang, Hui-Juan,Hu, Jing,Hu, Jian,Yang, Sheng-Yong,Zhao, Ying-Lan
, p. 7620 - 7636 (2015)
A series of quinoline derivatives was synthesized and biologically evaluated as Enhancer of Zeste Homologue 2 (EZH2) inhibitors. Structure-activity relationship (SAR) studies led to the discovery of 5-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinolin-4-amine (5k), which displayed an IC50 value of 1.2 μM against EZH2, decreased global H3K27me3 level in cells and also showed good anti-viability activities against two tumor cell lines. Due to the low molecular weight and the fact that no quinoline derivative has been reported as an EZH2 inhibitor, this compound could serve as a lead compound for further optimization.
A Convenient Preparation of 4,8-Dimethoxy-3-substituted-2(1H)-quinolones by an Electrophilic Reaction through Base-induced Deprotonation and its Synthetic Application for the Synthesis of New Alkaloids, 3,4,8-Trimethoxy-2(1H)-quinolone and 3-Formyl-4,7,8-trimethoxy-2(1H)-quinolone(Glycocitridine)
Tagawa, Yoshinobu,Kawaoka, Takamitsu,Goto, Yoshinobu
, p. 1677 - 1683 (2007/10/03)
Some 4,8-dimethoxy-3-substituted-2(1H)-quinolones were prepared by electrophilic reaction of 4,8-dimethoxy-2(1H)-quinolone with electrophiles in the presence of n-butyllithium-N,N,N',N',-tetramethylethylenediamine in fairly good yields. This present method was successfully applied for the synthesis of two new alkaloids bearing the 4,8-dimethoxy-2(1H)-quinolone skeleton.
