139039-23-9Relevant academic research and scientific papers
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)
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.
Polymer complexes XIX. Structural chemistry of poly(2-acrylamido-1,2-diaminobenzene) complexes
El-Sonbati, A. Z.,Diab, M. A.,Kotb, M. F.,Killa, H. M.
, p. 623 - 626 (2007/10/02)
New poly(2-acrylamido-1,2-diaminobenzene) homopolymer (PADB) reacts wit Cu(II), Ni(II), Zn(II), and UO2(+2) to give polymer complexes with different stoichiometry, depending on the metal salt and the reaction conditions.The polymer complexes have been cha
