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Contributor Information

  • Name Malcolm F G Stevens
  • Institute University of Nottingham

Tool Details

  • Tool name: Antitumoral Quinol1h Small Molecule (Tool Compound)
  • Molecular formula: C20H14FNO4S
  • Tool type: Small molecules
  • Tool sub-type: Antitumoral
  • Molecular weight of the target: 383.4
  • Application: Antitumor activity observed in HCT 116 (GI50 = 40 nM) and HT 29 (GI50 = 380 nM), and in breast cancer cell lines. Potent inhibitory effect in NCI 60 cells (GI50 =16 nM and LC50 = 2.24 ÂľM).
  • Description: A new class of molecule (4-hydroxy-4-hetarylcyclohexa-2,5-dien-1-ones) bearing a new pharmacophore (quinols') has been identified with potent activity against renal, colon and breast cell lines in the NCI 60-cell panel.
  • Research area: Cell Cycle; Epigenetics & Nuclear Signalling
  • IUPAC: 4-(1-Benzenesulfonyl-6-fluoro-1Hindol-2-yl)-4-hydroxy-cyclohexa-2,5-dienone
  • Additional notes: Exhibits a mean GI50 value of 16 nM and a mean LC50 value of 2.24 uM in the NCI 60- cell-line screen, with LC50 activity in the HCT 116 human colon cancer cell line below 10 nM. Compound available for screening or similar studies. For larger quantities (>20mg) please contact Ximbio.

  • For Research Use Only

Target Details

  • Target molecular weight: 383.4
  • Primary target: Thioredoxin reductase

Application Details

  • Application: Antitumor activity observed in HCT 116 (GI50 = 40 nM) and HT 29 (GI50 = 380 nM), and in breast cancer cell lines. Potent inhibitory effect in NCI 60 cells (GI50 =16 nM and LC50 = 2.24 ÂľM).

Handling

  • Purity: 383.4 g/mol
  • Solubility: DMSO to 100 mM
  • Storage conditions: -20°C (desiccating conditions)
  • Shipping conditions: Dry Ice

Documentation

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References

  • •  Chew et al. 2008. FASEB J. 22(6):2072-83. PMID: 18180330.
  • •  Thioredoxin reductase inhibition by antitumor quinols: a quinol pharmacophore effect correlating to antiproliferative activity.
  • •  Berry et al. 2005. J Med Chem. 48(2):639-44. PMID: 15658878.
  • •  Quinols as novel therapeutic agents. 2.(1) 4-(1-Arylsulfonylindol-2-yl)-4-hydroxycyclohexa-2,5-dien-1-ones and related agents as potent and selective antitumor agents.
  • •  Wells et al. 2003. J Med Chem. 46(4):532-41. PMID: 12570375.
  • •  4-Substituted 4-hydroxycyclohexa-2,5-dien-1-ones with selective activities against colon and renal cancer cell lines.