Synthesis and biological activities of truncated acridone: Structure-activity relationship studies of cytotoxic 5-hydroxy-4-quinolone

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 and antiherpes activities. Among them 5-hydroxy-8-methoxy-quinolone showed potent antitumor activity (IC 50 = 17.7 μM for HL60) which was gre...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 1997-04, Vol.7 (7), p.789-792
Main Authors: Woo Chun, Moon, Kim Olmstead, Kay, Suck Choi, Yong, Ock Lee, Chong, Lee, Chong-Kyo, Hyup Kim, Joong, Lee, Jeewoo
Format: Article
Language:English
Subjects:
Antineoplastic agents
Biological and medical sciences
General aspects
Medical sciences
Pharmacology. Drug treatments
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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 and antiherpes activities. Among them 5-hydroxy-8-methoxy-quinolone showed potent antitumor activity (IC 50 = 17.7 μM for HL60) which was greater than that of acronycine. 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 and antiherpes activities. Among them 5-hydroxy-8-methoxy-quinolone showed potent antitumor activity (IC 50 = 17.7 μM for HL60) which was greater than that of acronycine.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(97)00117-0