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Aryl phenolic compounds, Synthesis and uses

5-LOX inhibitorsAntinflammatorycancerCancroMultitargetPI3K/AKT/mTOR


The invention relates to the development of new leads compounds in anti-inflammatory and anti-cancer drug discovery, in particular the patent describe a convenient synthetic method for producing biologically active compounds, based on naturally occurring molecules,  with general formula (I) as 5-LOX and PI3K/AKT/mTOR pathway inhibitors. The drug is unique and with multiple action, thus overcoming the limitation of individual drugs; furthermore there is limited risk of interaction between different drugs (with consequent side / toxic effects) and greater simplicity of administration to the patient.

Technical features

In the general formula (I) X and Y are OH or H; Ar is directly linket to: phenyl, benzofuranyl, benzothiophenyl, nafthyl, triatenyl, antracenyl, dibenzofuranyl ring. Lead compounds from the synthetic library demonstrated anti-inflammatory and anti-cancer activities as multitarget compounds. Anticancer agents that modulate multiple pathways are preferred as they can better target cross-talks leading to activation of compensatory signaling, which allow cancer cells to evade apoptosis. Thus, combined inhibition of PI3-K/Akt and mTOR pathways seems to be a more efficient way of suppressing cancer cell growth and viability than targeting the components of each pathway alone.

Possible Applications

  • Treatment of Inflammation-related chronic diseases;
  • Drugs able to ameliorate inflammation response and oxidative stress in diseases;
  • Anticancer drug in solid tumors.


  • Multitarget compounds;
  • Discovery of new generation of anti-cancer/antinflammatory drugs, able to inhibit more than one pathway;
  • More predictive pharmacokinetics;
  • Better patient compliance;
  • Reduced risk of drug interactions.