Abstract
Here we report a number of novel JS-K structural analogues with sub-micromolar anti-proliferative activities against human leukemia cell lines HL-60 and U937; JS-K is the anti-cancer lead compound O(2)-(2,4-dinitrophenyl) 1-[(4-ethoxycarbonyl)piperazin-1-yl]diazen-1-ium-1,2-diolate. The ability of these compounds to generate intracellular nitric oxide correlated well with their observed anti-proliferative effects: analogues that had potent inhibitory activity against leukemia cells formed elevated levels of intracellular nitric oxide.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, N.I.H., Intramural
MeSH terms
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology
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Azo Compounds / chemical synthesis
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Azo Compounds / chemistry*
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Azo Compounds / pharmacology
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Cell Line, Tumor
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Humans
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Nitric Oxide / metabolism
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Piperazines / chemical synthesis
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Piperazines / chemistry*
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Piperazines / pharmacology
Substances
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Antineoplastic Agents
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Azo Compounds
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O(2)-(2,4-dinitrophenyl) 1-((4-ethoxycarbonyl)piperazin-1-yl)diazen-1-ium-1,2-diolate
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Piperazines
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Nitric Oxide