Y. Xia et al., Antitumor agents. 211. Fluorinated 2-phenyl-4-quinolone derivatives as antimitotic antitumor agents, J MED CHEM, 44(23), 2001, pp. 3932-3936
Fluorinated 2-phenyl-4-quinolone derivatives were synthesized and evaluated
in National Cancer Institute's 60 human tumor cell line in vitro screen. F
rom the results, the ketone moiety plays an essential role in activity. Amo
ng the compounds tested, 2'-fluoro-6-pyrrol-2-phenyl-4-quinolone (13) exhib
ited the most potent cytotoxic activities (log GI(50) < -8.00) against rena
l and melanoma tumor cell lines. Compound 13 was also a potent inhibitor of
tubulin polymerization (IC50 = 0.46 muM) and of radiolabeled colchicine bi
nding to tubulin, with activities comparable to those of the potent antimit
otic natural products colchicine, podophyllotoxin, and combretastatin A-4.