Synthesis and in vitro anti-leukemic activity of structural analogues of JS-K, an anti-cancer lead compound

Bioorg Med Chem Lett. 2008 Feb 1;18(3):950-3. doi: 10.1016/j.bmcl.2007.12.044. Epub 2008 Jan 4.

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

  • Research Support, N.I.H., Extramural
  • Research Support, N.I.H., Intramural

MeSH terms

  • Anti-Inflammatory Agents, Non-Steroidal / chemistry
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology
  • Antineoplastic Agents* / chemical synthesis
  • Antineoplastic Agents* / chemistry
  • Antineoplastic Agents* / pharmacology
  • Azo Compounds* / chemical synthesis
  • Azo Compounds* / chemistry
  • Azo Compounds* / pharmacology
  • Combinatorial Chemistry Techniques
  • Glutathione / metabolism
  • Glutathione Transferase / metabolism*
  • HL-60 Cells
  • Humans
  • Leukemia / metabolism
  • Models, Molecular
  • Molecular Structure
  • Nitric Oxide Donors / chemistry
  • Nitric Oxide Donors / pharmacology
  • Piperazines* / chemical synthesis
  • Piperazines* / chemistry
  • Piperazines* / pharmacology
  • Prodrugs / pharmacology

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Antineoplastic Agents
  • Azo Compounds
  • Nitric Oxide Donors
  • O(2)-(2,4-dinitrophenyl) 1-((4-ethoxycarbonyl)piperazin-1-yl)diazen-1-ium-1,2-diolate
  • Piperazines
  • Prodrugs
  • Glutathione Transferase
  • Glutathione