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Antitumoral Quinol1h Small Molecule (Tool Compound)

Invented at University of Nottingham

Info

Catalogue Number 151834
Antigen/Gene or Protein Targets Thioredoxin reductase
Type Antitumoral
Relevance 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.
Molecular Formula C20H14FNO4S
lUPAC 4-(1-Benzenesulfonyl-6-fluoro-1Hindol-2-yl)-4-hydroxy-cyclohexa-2,5-dienone
Molecular Weight (g/mol) 383.40
In vitro applications 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 µM).
Solubility DMSO to 100 mM
Research Area Cancer
Storage -20C (desiccating conditions)
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.

References

There are 6 reference entries for this reagent.

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References: 6 entries

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.

Europe PMC ID: 18180330

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.

Europe PMC ID: 15658878

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.

Europe PMC ID: 12570375


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References: 6 entries

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.


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Inventor Information

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