Abstract
A series of novel analogues of 1,3-diarylprop-2-en-1-one (3a-m) were synthesized and evaluated for their inhibitory activity of FOX P3 gene expression and apoptosis in CD4+T cells that had been isolated from the spleen of 8 to 10 weeks old mice. The structure-activity relationship (SAR) of the R1 and R2 modification was studied to identify a candidate with the maximum potency. Of these compounds, 3d showed the highest inhibitory activity of FOX P3 gene expression and apoptosis (66.5 % inhibition at 10 μM). To the best of the authors’ knowledge this is the first report of 1,3- diarylprop-2-en-1-ones as regulators of FOX P3 gene expression.
Keywords: 1, 3-Diarylprop-2-en-1-one, pyrazole, FOX P3, anti-cancer.
Medicinal Chemistry
Title:Synthesis and Inhibitory Effects of Some Novel 1,3-diarylprop-2-en-1-one Analogues in Foxp3 Expression: A Novel Class of Anti-cancer Candidates
Volume: 9 Issue: 8
Author(s): Mayank Kinger, Jeong Hoon Park, Min Goo Hur, Sang Wook Kim and Seung Dae Yang
Affiliation:
Keywords: 1, 3-Diarylprop-2-en-1-one, pyrazole, FOX P3, anti-cancer.
Abstract: A series of novel analogues of 1,3-diarylprop-2-en-1-one (3a-m) were synthesized and evaluated for their inhibitory activity of FOX P3 gene expression and apoptosis in CD4+T cells that had been isolated from the spleen of 8 to 10 weeks old mice. The structure-activity relationship (SAR) of the R1 and R2 modification was studied to identify a candidate with the maximum potency. Of these compounds, 3d showed the highest inhibitory activity of FOX P3 gene expression and apoptosis (66.5 % inhibition at 10 μM). To the best of the authors’ knowledge this is the first report of 1,3- diarylprop-2-en-1-ones as regulators of FOX P3 gene expression.
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Cite this article as:
Kinger Mayank, Park Hoon Jeong, Hur Goo Min, Kim Wook Sang and Yang Dae Seung, Synthesis and Inhibitory Effects of Some Novel 1,3-diarylprop-2-en-1-one Analogues in Foxp3 Expression: A Novel Class of Anti-cancer Candidates, Medicinal Chemistry 2013; 9 (8) . https://dx.doi.org/10.2174/15734064113099990029
DOI https://dx.doi.org/10.2174/15734064113099990029 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
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