Posters

      6-Aryl-β-Carbolines As Potent Tubulin-Polymerization Inhibitors

      Blaney, P.; Foster, S.; Blaney, E.; Hallworth, S.; Smith, A.; Doyle, P.; Fisher, R.; Teichert, A.; Lang, G.; Demotz, S.; McHugh, D.; Pospisil, P.; Goffman, F.
      Conference date
      May 9, 2013
      Conference name
      Grasmere Heterocyclic and Synthesis Meeting (RSC)
      Summary

      Natural products have proven to be an excellent resource for discovering new potential drug candidates. For example, a recent study has shown that 64% of anti-cancer drugs and 76% of anti-bacterial drugs are natural products or derivatives. 1. Within a program aimed at the exploration of the biological activities of semisynthetic libraries based on natural product scaffolds – one of which was harmane 1 – 6-aryl-β-carbolines 2. Were identified as potent cytotoxic agents with an in vivo anti-tumour activity. The underlying mechanism was found to be microtubulin depolymerization by interaction with the colchicine binding site.