Rationally designed less toxic SPD-304 analogs and preliminary evaluation of their TNF inhibitory effects.

@article{Alexiou2014RationallyDL,
  title={Rationally designed less toxic SPD-304 analogs and preliminary evaluation of their TNF inhibitory effects.},
  author={Polyxeni Alexiou and Athanasios Papakyriakou and Evangelos Ntougkos and Christos P. Papaneophytou and Fotini Liepouri and Anthi K Mettou and Ioannis Katsoulis and Anna Maranti and Katerina Tsiliouka and Alexandros T. Strongilos and Sotiria Chaitidou and Eleni Douni and George Kontopidis and George Kollias and Elias A. Couladouros and Elias Eliopoulos},
  journal={Archiv der Pharmazie},
  year={2014},
  volume={347 11},
  pages={
          798-805
        }
}
SPD-304 was discovered as a promising tumor necrosis factor alpha (TNF) antagonist that promotes dissociation of TNF trimers and therefore blocks the interaction of TNF and its receptor. However, SPD-304 contains a potentially toxic 3-alkylindole moiety, which can be bioactivated to a reactive electrophilic intermediate. A series of SPD-304 analogs was synthesized with the aim to diminish its toxicophore groups while maintaining the binding affinity for TNF. Incorporation of electron… CONTINUE READING

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