91004-38-5Relevant articles and documents
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
, 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.
Bulbiferates A and B: Antibacterial Acetamidohydroxybenzoates from a Marine Proteobacterium, Microbulbifer sp.
Jayanetti, Dinith R.,Braun, Doug R.,Barns, Kenneth J.,Rajski, Scott R.,Bugni, Tim S.
, p. 1930 - 1934 (2019/06/17)
Here we report the discovery of two new 3-acetamido-4-hydroxybenzoate esters, bulbiferates A (1) and B (2), isolated from Microbulbifer sp. cultivated from the marine tunicate Ecteinascidia turbinata. The structures of 1 and 2 were determined by analysis
Preparation method of Neratinib intermediate
-
Paragraph 0035-0036, (2017/11/29)
The invention relates to the field of chemical synthesis, and specifically relates to a preparation method of a Neratinib intermediate. A compound (I) is taken as the raw material, and through a series of reactions, the intermediate compound (VIII) of a novel antitumor drug Neratinib is obtained. A high efficient synthesis route is provided and has the characteristics of low cost, few byproducts, high yield, and little environmental pollution.
Design, synthesis and biological evaluation of novel pyrimidine, 3-cyanopyridine and m-amino-N-phenylbenzamide based monocyclic EGFR tyrosine kinase inhibitors
Mao, Yongjun,Zhu, Wenxiu,Kong, Xiaoguang,Wang, Zhen,Xie, Hua,Ding, Jian,Terrett, Nicholas Kenneth,Shen, Jingkang
, p. 3090 - 3104 (2013/07/11)
36 new compounds with the typical skeleton of 4-anilino-5-vinyl/ethynyl pyrimidine, 4-anilino-3-cyano-5-vinyl/ethynyl/phenyl pyridine, and m-amino-N-phenylbenzamide, are designed, synthesized and selectively tested on EGFR, ErbB-2 kinases, and A-549, HL60 cells growth inhibition. Results from the bioactivity and chemical structures yield preliminary structure-activity relationships (SARs). The most potent 5-ethynylpyrimidine derivative 20a has an IC50 value of 45 nM to EGFR kinase. Several compounds of other series also show IC50 values 1 μM for EGFR and 5 μM for A-549 and HL60 cells growth inhibition.