Modulation of Nad(P)H:quinone oxidoreductase (NQO1) activity mediated by 5-arylamino-2-methyl-4,7-dioxobenzothiazoles and their cytotoxic potential.
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.
Ryu
C K
CK
College of Pharmacy, Ewha Womans University, Seoul, Korea. ckryu@mm.ewha.ac.kr
Jeong
H J
HJ
Lee
S K
SK
Kang
H Y
HY
Ko
K M
KM
Sun
Y J
YJ
Song
E H
EH
Hur
Y H
YH
Lee
C O
CO
D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D004354:Drug Screening Assays, Antitumor; D004448:Echinomycin / Q000031:analogs & derivatives*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology*; D006801:Humans; D016660:NAD(P)H Dehydrogenase (Quinone) / Q000037:antagonists & inhibitors*; D011808:Quinone Reductases / Q000138:chemical synthesis* / Q000494:pharmacology; D013844:Thiazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D013844:Thiazoles; C010777:quinomycin; D004448:Echinomycin; D016660:NAD(P)H Dehydrogenase (Quinone); D011808:Quinone Reductases