Cytotoxic activity toward KB cells of 2-substituted naphtho[2,3-b]furan-4,9-diones and their related compounds.
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).
Ogawa
Masayuki
M
Faculty of Pharmaceutical Sciences, Josai University, Saitama, Japan.
Koyanagi
Jyunichi
J
Sugaya
Aiko
A
Tsuda
Tadashi
T
Ohguchi
Hiromi
H
Nakayama
Kouji
K
Yamamoto
Katsumi
K
Tanaka
Akira
A
D049109:Cell Proliferation / Q000187:drug effects; D006801:Humans; D007624:KB Cells; D015394:Molecular Structure; D009285:Naphthoquinones / Q000737:chemistry* / Q000633:toxicity*; D013329:Structure-Activity Relationship
D009285:Naphthoquinones; C073872:naphtho(2,3-b)furan-4,9-dione