• Title/Summary/Keyword: 5-Arylamino-2-methyl-4,7-dioxobenzothiazoles

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Synthesis and antifungal activity of 6-arylthio-/6-arylamino-4,7-dioxobenzothiazoles

  • Han, Ja-Young;Choi, Ik-Hwa;Chae, Mi-Jin;Jung, Ok-Jai;Ryu, Chung-Kyu
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.178.1-178.1
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    • 2003
  • 6-Arylthio-/6-arylamino-4,7-dioxobenzothiazoles were synthesized and tested for in vitro antifungal activity against Candida species and Aspergillus niger. 6-Arylamino-4,7-dioxobenzothiazoles showed, in general, more potent antifungal activity than 6-arylthio-4,7-dioxobenzothiazoles. The 6-arylamino-substituted compounds exhibited the greatest activity. In contrast, 6-arylthio-, 2-/5-methyl-or 5-methoxy-moieties of compounds did not improve their antifungal activity significantly. The results of this study suggest that 6-arylamino-4,7-dioxobenzothiazoles would be potent antifungal agents

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Modulation of NAD(P)H:Quinone Oxidoreductase (NQO1) Activity Mediated by 5-Arylamino-2-methyl -4,7-dioxobenzothiazoles and their Cytotoxic Potential

  • Ryu, Chung-Kyu;Jeong, Hyeh-Jean;Lee, Sang-Kook;Kang, Hye-Young;Ko, Kyung-Min;Sun, Yang-Jung;Song, Eun-Ha;Hur, Yeon-Hoe;Lee, Chong-Ock
    • Archives of Pharmacal Research
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    • v.23 no.6
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    • pp.554-558
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    • 2000
  • Synthesized 5-arylamino-2-methyl-4,7-dioxobenzothiazoles 3a-3o were evaluated for modulation of NAD(P)H: quinone oxidoreductase (NQOl) activity with the cytosolic fractions derived from cultured human lung cancer cells and their cytotoxicity in cultured several human solid cancer cell lines. The 4,7-dioxobenzothiazoles affected the reduction potential by NQOl activity and showed a potent cytotoxic activity against human cancer cell lines. The tested compounds 3a, 3b, 3g, 3h, 3n and 3o were considered as more potent cytotoxic agents, and comparable modulators of NQOl activity.

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