Modulation of Nad(P)H:quinone oxidoreductase (NQO1) activity mediated by 5-arylamino-2-methyl-4,7-dioxobenzothiazoles and their cytotoxic potential.

Abstract

Synthesized 5-arylamino-2-methyl-4,7-dioxobenzothiazoles 3a-3o were evaluated for modulation of NAD(P)H: quinone oxidoreductase (NQO1) 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 NQO1 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 NQO1 activity.

• Authors: C K Ryu, H J Jeong, S K Lee, H Y Kang, K M Ko, Y J Sun, E H Song, Y H Hur, C O Lee
• Journal: Archives of pharmacal research (Arch Pharm Res) Vol. 23 Issue 6 Pg. 554-8 (Dec 2000) ISSN: 0253-6269 [Print] Korea (South)
• PMID: 11156173 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Antineoplastic Agents
• Enzyme Inhibitors
• Thiazoles
• quinomycin
• Echinomycin
• NAD(P)H Dehydrogenase (Quinone)
• Quinone Reductases

Topics

• Antineoplastic Agents (chemical synthesis, pharmacology)
• Drug Screening Assays, Antitumor
• Echinomycin (analogs & derivatives)
• Enzyme Inhibitors (chemical synthesis, pharmacology)
• Humans
• NAD(P)H Dehydrogenase (Quinone) (antagonists & inhibitors)
• Quinone Reductases (chemical synthesis, pharmacology)
• Thiazoles (chemical synthesis, pharmacology)
• Tumor Cells, Cultured