Biological activity of 3-formylchromones and related compounds.

Masami Kawase, Toru Tanaka, Hiroyuki Kan, Satoru Tani, Hideki Nakashima, Hiroshi Sakagami

Index: In Vivo 21(5) , 829-34, (2007)

Full Text: HTML

Abstract

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.