2. Academic Validation
  3. 4-Carbonyl-2,6-dibenzylidenecyclohexanone derivatives as small molecule inhibitors of STAT3 signaling pathway

4-Carbonyl-2,6-dibenzylidenecyclohexanone derivatives as small molecule inhibitors of STAT3 signaling pathway

  • Bioorg Med Chem. 2016 Dec 1;24(23):6174-6182. doi: 10.1016/j.bmc.2016.09.070.
Peng Ji 1,  Congmin Yuan 2,  Shuhua Ma 3,  Junchao Fan 1,  Wei Fu 2,  Chunhua Qiao 1
Affiliations

Affiliations

  • 1 Department of Medicinal Chemistry, College of Pharmaceutical Science, Soochow University, 199 Ren Ai Road, Suzhou 215123, PR China.
  • 2 Department of Medicinal Chemistry, School of Pharmacy, Fudan University, Shanghai 201203, PR China.
  • 3 Department of Chemistry, Jess and Mildred Fisher College of Science and Mathematics, Towson University, 8000 York Road, Towson, MD 21252, United States.
PMID: 27816267 DOI: 10.1016/j.bmc.2016.09.070
Abstract

Inhibition of STAT3 signaling pathway is proposed to be a promising strategy for Cancer treatment. In this study, a series of 4-carbonyl-2,6-dibenzylidenecyclohexanone derivatives were prepared and evaluated as Anticancer agents. The most potent compound 13r was discovered to exhibit antiproliferative activity against a broad rang of Cancer cell lines and relatively low cytotoxicity against normal human cells. Besides, 13r effectively suppressed STAT3 expression as well as phosphorylation, and surface plasmon resonance analysis confirmed the direct interaction of 13r with STAT3. Docking simulation showed that 13r could inhibit STAT3 by targeting SH2 domain. This study provided evidence for these compounds to be further developed as antitumor agents through inhibition of the STAT3 pathway.

Keywords

Antitumor; Apoptosis; Curcumin; Inhibitors; STAT3.

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