100388-41-8Relevant articles and documents
Synthesis and biological evaluation of morpholine-substituted diphenylpyrimidine derivatives (Mor-DPPYs) as potent EGFR T790M inhibitors with improved activity toward the gefitinib-resistant non-small cell lung cancers (NSCLC)
Song, Zhendong,Huang, Shanshan,Yu, Haiqing,Jiang, Yu,Wang, Changyuan,Meng, Qiang,Shu, Xiaohong,Sun, Hunjun,Liu, Kexin,Li, Yanxia,Ma, Xiaodong
, p. 329 - 339 (2017/04/11)
Potential new EGFRT790M inhibitors comprised of structurally modified diphenylpyrimidine derivatives bearing a morpholine functionality (Mor-DPPYs) were used to improve the activity and selectivity of gefitinib-resistant non-small cell lung cancer (NSCLC) treatment. This led to the identification of inhibitor 10c, which displayed high activity against EGFRT790M/L858R kinase (IC50?=?0.71?nM) and repressed H1975?cell replication harboring EGFRT790M mutations at a concentration of 0.037?μM. Inhibitor 10c demonstrated high selectivity (SI?=?631.9) for T790M-containing EGFR mutants over wild type EGFR, suggesting that it will cause less side effects. Moreover, this compound also shows promising antitumor efficacy in a murine EGFRT790M/L858R-driven H1975 xenograft model without affecting body weight. This study provides new potential lead compounds for further development of anti-NSCLC drugs.
Synthesis and Biological Activity of Novel 1-Substituted Phenyl-4-[N-[(2'-morpholinothoxy)phenyl]aminomethyl]-1H-1,2,3-Triazoles
Mao, Ming-Zhen,Li, Yu-Xin,Zhou, Yun-Yun,Chen, Wei,Liu, Tuan-Wei,Yu, Shu-Jing,Wang, Su-Hua,Li, Zheng-Ming
scheme or table, p. 695 - 699 (2012/04/17)
In an attempt to search for potent antifungal agents, a series of novel 1-substituted phenyl-4-[N-[(2'-morpholinothoxy)phenyl]aminomethyl]-1H-1,2,3-triazoles 5a-m was designed and synthesized via Huisgen cycloaddition reaction between various (2-morpholin