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 HL60) which was greater than that of acronycine. However, these compounds didn't show any significant antiherpes or antituberculosis activity.
Chun
M W
MW
College of Pharmacy, Seoul National University, Korea.
Olmstead
K K
KK
Choi
Y
Y
Lee
C O
CO
Lee
C K
CK
Kim
J H
JH
Lee
J
J
D000166:Acridines / Q000737:chemistry*; D054831:Acridones; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D000998:Antiviral Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D004146:Dioxanes / Q000737:chemistry; D004354:Drug Screening Assays, Antitumor; D018259:Herpesvirus 1, Human / Q000187:drug effects; D018258:Herpesvirus 2, Human / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects; D011804:Quinolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
D000166:Acridines; D054831:Acridones; D000970:Antineoplastic Agents; D000998:Antiviral Agents; D004146:Dioxanes; D011804:Quinolines; C041300:acridone; C076489:Meldrum's acid