Abstract
Structural analogues of JS-K, an anti-cancer lead compound, were prepared and their in vitro anti-leukemic activity was determined. The rate of nitric oxide release from the corresponding diazeniumdiolate anions did not appear to affect the anti-leukemic activity of the prodrug forms. Two compounds with potent inhibitory activity and a potentially favorable toxicological profile were identified.
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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Anti-Inflammatory Agents, Non-Steroidal / chemistry
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Anti-Inflammatory Agents, Non-Steroidal / pharmacology
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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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Combinatorial Chemistry Techniques
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Glutathione / metabolism
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Glutathione Transferase / metabolism*
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HL-60 Cells
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Humans
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Leukemia / metabolism
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Models, Molecular
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Molecular Structure
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Nitric Oxide Donors / chemistry
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Nitric Oxide Donors / pharmacology
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Piperazines* / chemical synthesis
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Piperazines* / chemistry
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Piperazines* / pharmacology
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Prodrugs / pharmacology
Substances
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Anti-Inflammatory Agents, Non-Steroidal
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Antineoplastic Agents
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Azo Compounds
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Nitric Oxide Donors
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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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Prodrugs
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Glutathione Transferase
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Glutathione