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Synthesis and biological activity of 5-hydroxy-4-quinolones and 5-methoxy-4-quinolones as truncated acridones |
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| Authors: | Moon Woo Chun Kay Kim Olmstead Yongseok Choi Chong Ock Lee Chong-Kyo Lee Joong Hyup Kim Jeewoo Lee |
| Affiliation: | (1) College of Pharmacy, Seoul National University, Shinlim-Dong, Kwanak-Ku, 151-742 Seoul, Korea;(2) La Jolla Pharmaceutical Co., 6455 Nancy Ridge Drive, 92129 San Diego, CA, USA;(3) Korea Research Institute of Chemical Technology, Yusung, P.O. Box 107, 305-606 Taejeon, Korea;(4) Korea Institute of Science and Technology, Cheongryang, P.O. Box 130-650, 130-650 Seoul, Korea |
| Abstract: | 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 μM for HL60) which was greater than that of acronycine. However, these compounds didn't show any significant antiherpes or antituberculosis activity. |
| Keywords: | Acridone 5-hydroxy-4-quinolone 5-methoxy-4-quinolone Antitumor activity Antiherpes activity Antituberculosis activity |
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