Generic placeholder image

Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1573-4064
ISSN (Online): 1875-6638

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

Author(s): Mayank Kinger, Jeong Hoon Park, Min Goo Hur, Sang Wook Kim and Seung Dae Yang

Volume 9, Issue 8, 2013

Page: [1035 - 1040] Pages: 6

DOI: 10.2174/15734064113099990029

Price: $65

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.


Rights & Permissions Print Cite
© 2024 Bentham Science Publishers | Privacy Policy