Synthesis and structure‑activity‑relationship of 3,4‑Diaryl‑1H‑pyrrolo[2,3‑b]pyridines as irreversible Inhibitors of mutant EGFR‑L858R/T790M

Add time:07/14/2019    Source:sciencedirect.com

The epidermal growth factor receptor (EGFR) is a well‑validated drug target for the treatment of non‑small cell lung cancer. Here we present an optimization approach and preliminary structure‑activity relationship for 1H‑pyrrolo[2,3‑b]pyridines as covalent irreversible mutant EGFR inhibitors. We synthesized a focused library to investigate the effect of different aromatic substituents in the 4‑position of this scaffold, interacting with the gatekeeper. We determined the activity of the synthesized compounds mutant EGFR enzyme assays and determined the selectivity over the wild type.

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