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Preparation of Some Novel Trisubstituted 1,3,5-Triazines and Hybrid Linker Mode 1,3,5-Triazine Derivatives and Their Biological Evaluation

2019; Elsevier BV; Volume: 98; Issue: 4 Linguagem: Inglês

10.3987/com-19-14052

1881-0942

Kunihiro Sumoto, Nobuko Mibu, Kazumi Yokomizo, Junko Matsuyama, Syoko Tomonaga, Izumi Sakai, Yuki Kawano, Yumemi Matsumoto, Yuka Fujita, Yusuke Inoue, Masaya Iida, Kaneto Hashiguchi, Jianrong Steve Zhou, Makoto Furutachi, Kanae Yamada, Ryo Sato,

DNA and Nucleic Acid Chemistry

We report a new route to the preparation of C3-symmetrical multivalent hybrid-type molecules having a tris-aminoethylamine (TAEA) linker group and 1,3,5-triazine recognition moieties in the molecule and we also report the results of biological evaluation of their anti-herpes simplex virus type 1 (anti-HSV-1) activity and cytotoxic activity against Vero cells.Among the tested compounds, a new mid-size C2-symmetrical multivalent hybrid-type molecule (10aq) showed a high level of anti-HSV-1 activity (EC50 = 19.7 μM) with low cytotoxicity (CC50 > 200 μM) against Vero cells.A new CS-symmetrical multivalent derivative (4ab) also showed high anti-HSV-1 activity (EC50 = 1.77 μM) with low cytotoxicity (CC50 > 200 μM).The hybrid-type C2-symmetrical multivalent mid-size molecule (10aq) seems to be an interesting new lead in the search for new hybrid-type symmetrical multivalent antiviral compounds.