3987-92-6Relevant articles and documents
Design, synthesis and biological evaluation: 5-amino-1h-pyrazole-1-carbonyl derivatives as fgfr inhibitors
Zhang, Yan,Yu, Niefang
, p. 1330 - 1341 (2020/10/06)
Background: Fibroblast growth factors (FGFs) and their high affinity receptors (FGFRs) play a major role in cell proliferation, differentiation, migration, and apoptosis. Aberrant FGFR signaling pathway might accelerate development in a broad panel of mal
Identification of ortho-hydroxy anilide as a novel scaffold for lysine demethylase 5 inhibitors
Jaikhan, Pattaporn,Buranrat, Benjaporn,Itoh, Yukihiro,Chotitumnavee, Jiranan,Kurohara, Takashi,Suzuki, Takayoshi
supporting information, p. 1173 - 1176 (2019/03/29)
Fe(II)/α-ketoglutarate-dependent lysine demethylases (KDMs) are attractive drug targets for several diseases including cancer. In this study, we designed and screened ortho-substituted anilides that are expected to function as Fe(II) chelators, and identified ortho-hydroxy anilide as a novel scaffold for KDM5A inhibitors. Treatment of human lung cancer A549 cells with a prodrug form of 4-carboxy-2-hydroxy-formanilide (9c) increased trimethylated lysine 4 on histone H3 level, suggesting KDM5 inhibition in the cells.
Synthesis and biological evaluation of N-substituted 3-oxo-1,2,3,4-tetrahydro-quinoxaline-6-carboxylic acid derivatives as tubulin polymerization inhibitors
Qi, Jianguo,Dong, Haiyang,Huang, Jing,Zhang, Shufeng,Niu, Linqiang,Zhang, Yahong,Wang, Jianhong
, p. 8 - 20 (2017/11/23)
A series of novel N-substituted 3-oxo-1,2,3,4-tetrahydro-quinoxaline-6-carboxy- lic acid derivatives were synthesized and evaluated for their biological activities. Among all synthesized target compounds, 13d exhibited the most potent antiproliferative ac