Antitumor agents. 211. Fluorinated 2-phenyl-4-quinolone derivatives as antimitotic antitumor agents

Citation
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
Citations number
17
Categorie Soggetti
Chemistry & Analysis
Journal title
JOURNAL OF MEDICINAL CHEMISTRY
ISSN journal
00222623 → ACNP
Volume
44
Issue
23
Year of publication
2001
Pages
3932 - 3936
Database
ISI
SICI code
0022-2623(20011108)44:23<3932:AA2F2D>2.0.ZU;2-2
Abstract
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.