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Antitumoral Quinol2 Small Molecule (Tool Compound)

Invented at University of Nottingham

Info

Catalogue Number 151840
Antigen/Gene or Protein Targets Thioredoxin reductase
Type Inhibitor
Relevance 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
Molecular Formula C13H9NO2S
lUPAC 4-Benzothiazol-2-yl-4-hydroxycyclohexa-2,5-dienone
Molecular Weight (g/mol) 243.29
In vivo applications 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.
In vitro applications 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.
Research Area Cancer
Storage Ambient

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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