Mibu Nobuko, Yokomizo Kazumi, Murakami Kana, Ono Yurika, Ishimaru Masato, Otsubo Marie, Inao Hiroshi, Ono Yutaro, Zhou Jian-Rong, Sumoto Kunihiro
Faculty of Pharmaceutical Sciences, Fukuoka University.
Chem Pharm Bull (Tokyo). 2016;64(12):1769-1780. doi: 10.1248/cpb.c16-00682.
We report the preparation of new tripodal receptor-type C- and C-symmetrical molecules constructed on a tris(2-aminoethyl)amine (TAEA) template. Both the anti-herpes simplex virus type 1 (anti-HSV-1) activity and cytotoxic activity of synthesized receptor-type derivatives were evaluated in order to find a characteristic structural feature for these bioactivities of compounds. Among the compounds of synthesized symmetrical TAEA-related derivatives, compound 13k showed high anti-HSV-1 activity (50% effective concentration (EC)=16.7 µM) and low cytotoxicity (50% cytotoxic concentration (CC)=>200 µM). The presence of a hydrogen bond donor proton in the molecule is thought to be an important structural factor for expressing potential anti-HSV-1 activities.
我们报道了基于三（2-氨基乙基）胺（TAEA）模板构建的新型三脚架受体型C对称和C对称分子的制备。为了找到这些化合物生物活性的特征结构特征，对合成的受体型衍生物的抗1型单纯疱疹病毒（抗HSV-1）活性和细胞毒性活性进行了评估。在合成的对称TAEA相关衍生物的化合物中，化合物13k表现出高抗HSV-1活性（50%有效浓度（EC）=16.7µM）和低细胞毒性（50%细胞毒性浓度（CC）>200µM）。分子中氢键供体质子的存在被认为是表达潜在抗HSV-1活性的重要结构因素。
