Design, synthesis, and evaluation of peptidomimetics containing Freidinger lactams as STAT3 inhibitors

The STAT3 oncogene is a promising molecular target for the design of a new class of anticancer drugs. In this letter, we describe the design, synthesis, and evaluation of peptidomimetics containing Freidinger lactams as novel STAT3 inhibitors. Compound 3 binds to STAT3 with a Ki value of 190 nM and is a promising lead compound for further design and optimization.