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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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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.

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Correspondence to Moon Woo Chun.

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Chun, M.W., Olmstead, K.K., Choi, Y. et al. Synthesis and biological activity of 5-hydroxy-4-quinolones and 5-methoxy-4-quinolones as truncated acridones. Arch. Pharm. Res. 21, 445–451 (1998). https://doi.org/10.1007/BF02974641

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Key words

  • Acridone
  • 5-hydroxy-4-quinolone
  • 5-methoxy-4-quinolone
  • Antitumor activity
  • Antiherpes activity
  • Antituberculosis activity