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

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.

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