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


Authored by  P Blaney*, S Foster*, E Blaney*, S Hallworth*, A Smith*, P Doyle*, R Fisher*, A Teichert, G Lang, S Demotz, D McHugh, P Pospisil, FD Goffman

Presented at RSC ADVANCING THE CHEMICAL SCIENCES - HETEROCYCLIC & SYNTHESIS GROUP 21ST GRASMERE MEETING    
* This author is not affiliated with PMI.

Abstract

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. 

6-aryl-β-carbolines-as-potent-tubulin-polymerization-inhibitors