815-58-7Relevant articles and documents
Panzer,Suttle
, p. 244,245 (1960)
Design, synthesis and biological evaluation of AZD9291 derivatives as selective and potent EGFRL858R/T790M inhibitors
Zhao, Bingbing,Xiao, Zhen,Qi, Jianguo,Luo, Rong,Lan, Zhou,Zhang, Yanzhuo,Hu, Xiaohan,Tang, Qidong,Zheng, Pengwu,Xu, Shan,Zhu, Wufu
, p. 367 - 380 (2018/12/13)
Third-generation epidermal growth factor receptor (EGFR)L858R/T790M inhibitors are still the main drugs for the treatment of advanced non-small cell lung cancer (NSCLC), and these drugs have achieved remarkable clinical efficacy. However, there are still many patients suffering from drug-resistant mutations and drug side effects caused by NSCLC. In this study, guided by the molecular simulation, we applied a structure-based drug design strategy (SBDD) and optimized the structure to obtain a series of potent and selective EGFRL858R/T790M inhibitors. The most potent compound 18e demonstrated excellent kinase inhibitory activity and selectivity for EGFRL858R/T790M double mutants and the IC50 value reached nanomolar level. The selectivity of 18e against wild-type EGFR was near to 200-fold. In addition, compound 18e also inhibited H1975 cells proliferation at G2/M phase and induced apoptosis at a concentration of 0.25 μM, which makes it more valuable for potential lung cancer research.
Chemistry of polyhalogenated nitrobutadienes, 2: Synthesis of N-tetrachloroallylidene-N′-arylhydrazines by a formal synproportionation reaction
Zapol'skii, Viktor A.,Nutz, Eva,Namyslo, Jan C.,Adam, Arnold E. W.,Kaufmann, Dieter E.
, p. 2927 - 2933 (2008/02/05)
The reaction of 2-nitropentachlorobuta-1,3-diene with a variety of anilines substituted with electron-withdrawing groups generates, contrary to expectations, N-tetrachloroallylidene-N′-arylhydrazines instead of 1,1-bisaminated substitution products. The imidoyl-type chlorides are capable of undergoing nucleophilic substitution with amines or hydrides. The resulting compounds should exhibit physiological activity, especially for use in crop science. Georg Thieme Verlag Stuttgart.