Ogawa Masayuki, Koyanagi Jyunichi, Sugaya Aiko, Tsuda Tadashi, Ohguchi Hiromi, Nakayama Kouji, Yamamoto Katsumi, Tanaka Akira
Faculty of Pharmaceutical Sciences, Josai University, Saitama, Japan.
Biosci Biotechnol Biochem. 2006 Apr;70(4):1009-12. doi: 10.1271/bbb.70.1009.
We investigated the cytotoxic activity of 2-substituted naphtho[2,3-b]furan-4,9-diones. We have previously synthesized 33 types of 2-substituted and related compounds, and the cytotoxic activity of these compounds was then examined by a KB cell culture assay. 2-(3-Furanoyl)benzoic acids and 1,4-naphthoquinones had no activity. 2-Acetyl-4,9-dimethoxynaphtho[2,3-b]furan 4 showed low activity. However, parent naphtho[2,3-b]furan-4,9-dione 2 and most 2-substituted derivatives exhibited cytotoxic activity. The parent structure was therefore for cytotoxicity. 2-Formylnaphtho[2,3-b]furan-4,9-dione 11 had particularly potent activity (ED50=0.09 microg/ml).
我们研究了2-取代萘并[2,3-b]呋喃-4,9-二酮的细胞毒性活性。我们之前合成了33种2-取代及相关化合物，然后通过KB细胞培养试验检测了这些化合物的细胞毒性活性。2-(3-呋喃甲酰基)苯甲酸和1,4-萘醌没有活性。2-乙酰基-4,9-二甲氧基萘并[2,3-b]呋喃4表现出低活性。然而，母体萘并[2,3-b]呋喃-4,9-二酮2和大多数2-取代衍生物表现出细胞毒性活性。因此，母体结构具有细胞毒性。2-甲酰基萘并[2,3-b]呋喃-4,9-二酮11具有特别强的活性（半数有效剂量=0.09微克/毫升）。
