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新型对称三(2-氨乙基)胺衍生物的分子对称性与生物活性

Molecular symmetry and biological activities of new symmetrical tris(2-aminoethyl)amine derivatives.

作者信息

Mibu Nobuko, Yokomizo Kazumi, Uchida Wataru, Takemura Satoshi, Zhou Jianrong, Aki Hatsumi, Miyata Takeshi, Sumoto Kunihiro

机构信息

Faculty of Pharmaceutical Sciences, Fukuoka University, Fukuoka, Japan.

出版信息

Chem Pharm Bull (Tokyo). 2012;60(3):408-14. doi: 10.1248/cpb.60.408.

DOI:10.1248/cpb.60.408
PMID:22382425
Abstract

In terms of molecular symmetry and bioactivity, new C3- and CS-symmetrical derivatives based on the tris(2-aminoethyl)amine scaffold were designed and synthesized. The synthesized compounds were evaluated for antiviral activity with herpes simplex virus type 1 (HSV-1) by a plaque reduction assay and for cytotoxic activity with Vero cells. Most of the compounds showed no significant anti-HSV-1 activity, but some of the symmetrical derivatives showed high levels of cytotoxic activitiy.

摘要

在分子对称性和生物活性方面,设计并合成了基于三(2-氨基乙基)胺支架的新型C3和C5对称衍生物。通过蚀斑减少试验评估合成化合物对1型单纯疱疹病毒(HSV-1)的抗病毒活性,并通过对非洲绿猴肾细胞(Vero细胞)评估其细胞毒性活性。大多数化合物没有显示出显著的抗HSV-1活性,但一些对称衍生物显示出高水平的细胞毒性活性。

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