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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
Authors:Chung-Kyu Ryu  Hyeh-Jean Jeong  Sang Kook Lee  Hye-Young Kang  Kyung-Min Ko  Yang-Jung Sun  Eun-Ha Song  Yeon Hoe Hur  Chong-Ock Lee
Affiliation:College of Pharmacy, Ewha Womans University, Seoul, Korea. ckryu@mm.ewha.ac.kr
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.
Keywords:5-Arylamino-2-methyl-4,7-dioxobenzothiazoles  NAD(P)H  Quinone oxidoreductase (NQO1)  Cytotoxicity
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