Synthesis and biological activity of 5-hydroxy-4-quinolones and 5-methoxy-4-quinolones as truncated acridones

A series of 5-hydroxy-4-quinolone (3) and 5-methoxy-4-quinolone (4) derivatives were synthesized as truncated acridone analogues and evaluated for antitumor, antiherpes and antituberculosis activities. Among them 5-hydroxy-8-methoxy-quinolone showed potent antitumor activity (IC50 = 17.7 microM for...

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Published inArchives of pharmacal research Vol. 21; no. 4; pp. 445 - 451
Main Authors Chun, M W, Olmstead, K K, Choi, Y, Lee, C O, Lee, C K, Kim, J H, Lee, J
Format Journal Article
LanguageEnglish
Published Korea (South) 01.08.1998
Subjects
Acridines - chemistry
Acridones
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Antiviral Agents - chemical synthesis
Antiviral Agents - chemistry
Antiviral Agents - pharmacology
Dioxanes - chemistry
Drug Screening Assays, Antitumor
Herpesvirus 1, Human - drug effects
Herpesvirus 2, Human - drug effects
Microbial Sensitivity Tests
Mycobacterium tuberculosis - drug effects
Quinolines - chemical synthesis
Quinolines - chemistry
Quinolines - pharmacology
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Summary:A series of 5-hydroxy-4-quinolone (3) and 5-methoxy-4-quinolone (4) derivatives were synthesized as truncated acridone analogues and evaluated for antitumor, antiherpes and antituberculosis activities. Among them 5-hydroxy-8-methoxy-quinolone showed potent antitumor activity (IC50 = 17.7 microM for HL60) which was greater than that of acronycine. However, these compounds didn't show any significant antiherpes or antituberculosis activity.
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
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ISSN:0253-6269
1976-3786
DOI:10.1007/BF02974641