Antitumoral Quinol1h Small Molecule (Tool Compound)
- Name Malcolm F G Stevens
- Institute University of Nottingham
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
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
- • 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.