Biological activity of 3-formylchromones and related compounds.
Several 3-formylchromone derivatives were examined for their tumor cell-cytotoxic, anti-Helicobacter pylori, urease inhibitory and anti-HIV activity. Comparing their relative cytotoxicity against four human tumor cell lines and three normal human cells, tumor cell-specific cytotoxicity was detected in some 3-formylchromone derivatives. There was no clear-cut relationship between the cytotoxicity and the chemical structures of the compounds. 6,8-Dichloro-3-formylchromone (FC10) showed comparable anti-H. pylori activity with metronidazole and potent urease inhibition against jack bean urease. On the other hand, 6,8-dibromo-3-formylchromone (FC11) exhibited potent inhibitory activity against the urease, but had no anti-H. pylori activity. No chromones (FC1-16) exhibited anti-HIV activity.
Kawase
Masami
M
Faculty of Pharmaceutical Sciences, Matsuyama University, 4-2 Bunkyo-cho, Matsuyama, Ehime 790-8578, Japan. kawase@cc.matsuyama-u.ac.jp
Tanaka
Toru
T
Kan
Hiroyuki
H
Tani
Satoru
S
Nakashima
Hideki
H
Sakagami
Hiroshi
H
D000970:Antineoplastic Agents / Q000737:chemistry* / Q000633:toxicity*; D000998:Antiviral Agents / Q000737:chemistry* / Q000633:toxicity*; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D002867:Chromones / Q000737:chemistry* / Q000633:toxicity*; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology; D015497:HIV-1 / Q000187:drug effects; D016480:Helicobacter pylori / Q000187:drug effects; D006801:Humans; D015394:Molecular Structure; D014510:Urease / Q000037:antagonists & inhibitors / Q000378:metabolism
D000970:Antineoplastic Agents; D000998:Antiviral Agents; D002867:Chromones; D004791:Enzyme Inhibitors; C502480:formylchromone; D014510:Urease