68621-88-5Relevant articles and documents
Discovery and Structural Optimization of N5-Substituted 6,7-Dioxo-6,7-dihydropteridines as Potent and Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors against L858R/T790M Resistance Mutation
Hao, Yongjia,Wang, Xia,Zhang, Tao,Sun, Deheng,Tong, Yi,Xu, Yuqiong,Chen, Haiyang,Tong, Linjiang,Zhu, Lili,Zhao, Zhenjiang,Chen, Zhuo,Ding, Jian,Xie, Hua,Xu, Yufang,Li, Honglin
, p. 7111 - 7124 (2016)
EGFR-targeted inhibitors (gefitinib and erlotinib) provided an effective strategy for the treatment of non-small-cell lung cancer. However, the EGFR T790M secondary mutation has become a leading cause of clinically acquired resistance to these agents. Her
SARs of a novel series of s-triazine compounds targeting vimentin to induce methuotic phenotype
Zhang, Lei,Qu, Zhipeng,Wu, Jianping,Yao, Shining,Zhang, Qingqing,Zhang, Tao,Mo, Lian,Yao, Qizheng,Xu, Ying,Chen, Ruihuan
, (2021/02/09)
Herein, we describe the design, synthesis and structure?activity relationships of a series of novel s-triazine compounds can induce methuotic phenotype in various types of cancer cells. (E)-1-(4-Chlorophenyl)-3-(4-((4-morpholino-6-styryl-1,3,5-triazine-2-yl)amino)phenyl)urea, compound V6, exhibited a striking methuotic phenotype with a minimal effective concentration of less than 10 nM in U87 glioblastoma cells. Based on structure?activity relationship studies, we designed and synthesized an active probe P1 that retained the full potential of V6 in inducing the methuotic phenotype in U87 glioblastoma cells. Using this probe following affinity-based proteomic profiling strategy, we identified vimentin as the specific target protein of compound V6. Molecular docking revealed that V6 can form hydrogen bonds with vimentin at 273R and 276Y in its rod domain.
Various located urea and schiff-base bifunctional derivatives: Their gelation and Zn2+ sensing behaviors
Chen, Yu,Lei, Zhimei,Liu, Jie,Sun, He-Lue,Xing, Li-Juan,Yu, Haitao,Zhang, Xin
, (2020/09/16)
The efficient combination of various moieties is helpful to develop organic functional molecules. Herein, three of urea and Schiff-base bifunctional derivatives (OG, MG and PG) were prepared from o/m/p-diaminobenzene respectively. Benefitting from the urea and Schiff-base, these derivatives revealed satisfactory gelation capacity. However, the various locations of urea and imine paved them markedly different assembly performances during the gel formation. Additionally, these functional molecules displayed obvious “off-on” fluorescence sensing behaviors towards Zn2+ in solution ascribing to the imine and neighbor phenolic hydroxyl, among which the MG displayed the best Zn2+ selectivity. Crucially, the MG also realized Zn2+ probing at cellular level and its gel gave a visual detection via the gel-sol transition.