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.
Outcomes:
The project has ended successfully with 11 active compounds identified in in-vivo model. A 4th iteration is on-going.