0000000000874552
AUTHOR
Wengui Duan
Synthesis and Antitumor Evaluation of Menthone-Derived Pyrimidine-Urea Compounds as Potential PI3K/Akt/mTOR Signaling Pathway Inhibitor.
A series of novel menthone derivatives bearing pyrimidine and urea moieties was designed and synthesized to explore more potent natural product-derived antitumor agents. The structures of the target compounds were confirmed by FTIR, NMR, and HRMS. The in vitro antitumor activity was tested by standard methyl thiazolytetrazolium assay and showed that 4i, 4g, 4s, and 4m are the best compounds with IC50 values of 6.04 ± 0.62µM, 3.21 ± 0.67µM, 19.09 ± 0.49µM, and 18.68 ± 1.53µM, against Hela, MGC-803, MCF-7, and A549, respectively. The results of the preliminary action mechanism studies showed that compound 4i, the representative compound, could induce cell apoptosis in Hela cells in a dose-dep…
Crystal Structure and Host-Guest Binding Ability of Three Types of Pillar[5]arenes
A systematic research of the structural characterization and the host-guest binding abilities between three types of pillar[5]arenes 3–5 (3 for Structure Type I, 4 for Structure Type II and 5 for Structure Type III) is carried out by 1H NMR measurements and X-ray study. The results show that the configurations or symmetry of their cavities not only have large difference in these three types of pillar[5]arenes, but also have more or less variations even in the same structure type or the same host locked different guests such as crystals of 3a–3b, 4a–4d. On the other hand, the complexation behavior of pillar[5]arenes with 1,4-dibromobutane (DBB) is affected by the different symmetrical struct…