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KMID : 0043320010240050390
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Archives of Pharmacal Research
2001 Volume.24 No. 5 p.390 ~ p.396
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Effects of 6-Arylamino-5,8-quinolinediones and 6-Chlore-7-ary-lamino-5,8-isoquinolinediones on NAD(P)H : Quinone Oxidoreductase (NQO1 ) Activity and Their Cytotoxic Potential
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Ryu Chung-Kyu
Jeong Hyeh-Jean
Lee Sang-Kook
You Hee-Jung
Choi Ko-Un
Shim Ju-Yeon
Heo Yeon-Hoi
Lee Chong-Ock
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Abstract
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Synthesized 6-arylamino-5,8-quinolinediones 4a-4j and 6-chloro-7-arylamino-5,8-isoquinolinediones 5a-5g were evaluated for effects on 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 5,8-quinolinediones 4 and 5,8-isoquinolinediones 5 affected the reduction potential by NQO1 activity and showed a potent cytotoxic activity against human cancer cell lines. The tested compounds 4a, 5c, 5f, and 5g were considered as more potent cytotoxic agents. The compounds 4d, 5b, 5c, 5e and 5g were comparable modulators of NQO1 activity.
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KEYWORD
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6-Arylamino-5, 8-quinolinediones, 6-Chlore-7-ary-lamino-5, 8-isoquinolinediones, NAD(P)H, Quinone Oxidoreductase (NQO1 ), Cytotoxicity
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