Mayank Kinger, Jeong Hoon Park, Min Goo Hur, Sang Wook Kim and Seung Dae Yang Pages 1035 - 1040 ( 6 )
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.
1, 3-Diarylprop-2-en-1-one, pyrazole, FOX P3, anti-cancer.
Department of Advanced Materials Chemistry, College of Science and Technology, Dongguk University-Gyeongju, 780-714, Republic of Korea.