Pyrrole‐based EGFR inhibitors for the treatment of NCSLC: Binding modes and SARs investigations

Abstract

The treatment of advanced non‐small cell lung cancer (NSCLC) has made substantial progress due to the rapid development of small molecule targeted therapy, with dramatically prolonged survival. As an effective drug for the treatment of NSCLC, epidermal growth factor receptor (EGFR) inhibitors are currently experiencing issues like severe adverse events and drug resistance. It is urgent to develop novel types of EGFR inhibitors to overcome the abovementioned limitations. Pyrrole always works well as a probe for the creation of novel medication candidates for hard‐to‐treat conditions like lung cancer. Although the design, synthesis, and biological assays of pyrrole derivatives have been reported, their inhibitory actions against the receptor tyrosine kinase (RTK) EGFR have not been in‐depthly studied. This review highlights the small molecule EGFR inhibitors containing pyrrole heterocyclic pharmacophores in recent years, and the research on their mechanism, biological activity, and structure–activity relationship (SAR).

3-Trifluoromethyl Pyrrole Synthesis Based on β-CF3-1,3-Enynamides

“…The design and discovery of new reactions for the synthesis of pyrrole frameworks has been stimulated by the appearance of such frameworks in many bioactive natural products, commercial drugs, and functional materials . Moreover, pyrrole-based structures are versatile building blocks for the synthesis of value-added compounds .…”