This project proposes to screen additional CDRD chemical libraries in order to identify a greater number of unique compounds that inhibit FEN1 at low micromolar potency. In parallel, a complimentary medicinal chemistry program will be established around both the current inhibitors identified and inhibitors to be identified in the above screens in order to generate new IP on a series of pharmacophores. Future work will assess hits for toxicity and pharmacokinetic parameters and evaluate activity in cancer xenograft models.
The project has ended successfully with 11 active compounds identified in in-vivo model. A 4th iteration is on-going.