Abstract:
:As part of a continuing search for potential anticancer drug candidates in the 2-phenyl-4-quinolone series, 3',6-substituted 2-phenyl-4-quinolone-3-carboxylic acid derivatives and their salts were synthesized and evaluated. Preliminary screening showed that carboxylic acid analogs containing a m-fluoro substituted 2-phenyl group displayed the highest in vitro anticancer activity. Activity decreased significantly if a chlorine or methoxy group replaced the fluorine atom. 3'-Fluoro-6-methoxy-2-phenyl-4-quinolone-3-carboxylic acid (68) had the highest in vitro cytotoxic activity among all tested carboxylic acid derivatives and their salts. The mechanism of action may be similar, but not identical, to that of tubulin binding drugs, such as navelbine and taxol. Compound 68 merits further investigation as a novel hydrophilic antimitotic agent.
journal_name
Bioorg Med Chemjournal_title
Bioorganic & medicinal chemistryauthors
Lai YY,Huang LJ,Lee KH,Xiao Z,Bastow KF,Yamori T,Kuo SCdoi
10.1016/j.bmc.2004.09.041subject
Has Abstractpub_date
2005-01-03 00:00:00pages
265-75issue
1eissn
0968-0896issn
1464-3391pii
S0968-0896(04)00738-2journal_volume
13pub_type
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