HETEROCYCLES

■ Some Hybrid Linker Mode C2-Symmetrical 1,3,5-Triazine Derivatives and Their Biological Evaluation

Nobuko Mibu, Makoto Furutachi, Yusuke Inoue, Yuka Fujita, Yumemi Matsumoto, Yuki Kawano, Syoko Tomonaga, Junko Matsuyama, Kanae Yamada, Ryo Sato, Kazumi Yokomizo, Jian-Rong Zhou, Shunsuke Shimomura, Kaori Ota, and Kunihiro Sumoto*

*Faculty of Pharmaceutical Sciences, Fukuoka University, 8-19-1 Nanakuma, Jonan-ku, Fukuoka 814-0180, Japan

Abstract

We report the preparation of some new C2-symmetrical multivalent hybrid-type molecules having a methylene linker group and 1,3,5-triazine (TAZ) 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. All mid-size C2-symmetrical multivalent hybrid-type molecules (3a-2, 3a-4, 3b-2, 3b-3, 3b-4) showed considerably high levels of anti-HSV-1 activity (EC50 = 7.6 ~ 95.6 μM) with low levels of cytotoxicity (CC50 > 200 μM) against Vero cells. Among the tested compounds, the hybrid-type C2-symmetrical multivalent molecule (3a-4) seems to be an interesting new lead in the search for new hybrid-type multivalent mid-size antiviral compounds.