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Contributor Information

  • Name Malcolm F G Stevens
  • Institute University of Nottingham

Tool Details

  • Tool name: Antitumoral Quinol2 Small Molecule (Tool Compound)
  • Molecular formula: C13H9NO2S
  • Tool type: Small molecules
  • Tool sub-type: Inhibitor
  • Molecular weight of the target: 243.29
  • Application: Displays in vivo antitumor activity against human RXF 944XL renal xenografts in nude NMRI mice. Inhibits thioredoxin reductase with potencies correlated with their antiproliferative and cytotoxic efficacies. Potent activity against renal, colon, and breast cancer cell lines in the NCI 60-cell panel. Shows potent antitumor activity in HCT 116 and HT 29 human colon as well as MCF 7 and MDA 468 human breast cancer cell lines.
  • Description: The antitumoral Quinol2, also known as PMX464, is a potent in vitro antitumour activity was observed in HCT 116 and HT 29 human colon as well in as MCF-7 and MDA 468 human breast cancer cell lines. This molecule also showed in vivo antitumour activity against human RXF 944XL renal xenografts in nude NMRI mice.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. It also demonstrates potent in vitro anti-proliferative activity and in vivo anti-tumour activity in tumour xenografts
  • Research area: Cancer
  • IUPAC: 4-Benzothiazol-2-yl-4-hydroxycyclohexa-2,5-dienone

  • For Research Use Only

Target Details

  • Target molecular weight: 243.29
  • Primary target: Thioredoxin reductase

Application Details

  • Application: Displays in vivo antitumor activity against human RXF 944XL renal xenografts in nude NMRI mice. Inhibits thioredoxin reductase with potencies correlated with their antiproliferative and cytotoxic efficacies. Potent activity against renal, colon, and breast cancer cell lines in the NCI 60-cell panel. Shows potent antitumor activity in HCT 116 and HT 29 human colon as well as MCF 7 and MDA 468 human breast cancer cell lines.

Handling

  • Purity: 243.29 g/mol
  • Storage conditions: Ambient
  • 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.