300558-35-4Relevant academic research and scientific papers
Novel Quinazoline Derivatives Bearing Various 4-Aniline Moieties as Potent EGFR Inhibitors with Enhanced Activity Against NSCLC Cell Lines
Wang, Changyan,Sun, Yajun,Zhu, Xingqi,Wu, Bin,Wang, Qiao,Zhen, Yuhong,Shu, Xiaohong,Liu, Kexin,Zhou, Youwen,Ma, Xiaodong
, p. 635 - 643 (2016)
A class of novel quinazoline derivatives bearing various C-4 aniline moieties was synthesized and biologically evaluated as potent epidermal growth factor receptor (EGFR) inhibitors for intervention of non-small-cell lung cancer (NSCLC). Most of these inhibitors are comparable to gefitinib in inhibiting these cancer cell lines, and several of them even displayed superior inhibitory activity. In particular, analogue 5b with an IC50 of 0.10 μm against the EGFR wild-type A431 cells and 5c with an IC50 of 0.001 μm against the gefitinib-sensitive HCC827 cells (EGFR del E746-A750) was identified as highly active EGFR inhibitors. It was also significant that the discovered analogue 2f, not only has high potency against the gefitinib-sensitive cells (IC50 = 0.031 μm), but also possesses remarkably improved activity against the gefitinib-resistant cells. In addition, the enzymatic assays and the Western blot analysis for evaluating the effects of the typical inhibitors indicated that these molecules strongly interfere with the EGFR target.
P-tert-Butyl thiacalix[4]arenes functionalized at the lower rim by amide, hydroxyl and ester groups as anion receptors
Stoikov, Ivan I.,Yantemirova, Alena A.,Nosov, Roman V.,Rizvanov, Ildar Kh.,Julmetov, Ajdar R.,Klochkov, Vladimir V.,Antipin, Igor S.,Konovalov, Alexander I.,Zharov, Ilya
experimental part, p. 3225 - 3234 (2011/06/21)
New p-tert-butyl thiacalix[4]arenes differently substituted at the lower rim with amide, hydroxyl and ester groups were synthesized. Binding properties of the compounds toward some tetrabutylammonium salts n-Bu4NX (X = F-, Cl-, Br-, I-, CH 3CO2-, H2PO4-, NO3-) were studied by UV spectroscopy. It was found that the stoichiometry of the complexes, generally, is 1:1, and the association constants are in the range of 103-105 M-1. The p-tert-butyl thiacalix[4]arenes containing secondary amide groups trisubstituted at the lower rim bind the studied anions most effectively. Selective receptors for fluoride and dihydrogen phosphate salts of tetrabutylammonium were found.
