Tetracyclic pyrazinocarbazole derivatives as YAP-TEAD pathway inhibitors with activity in a melanoma lung colonization model.
Direct pharmacological disruption of the YAP-TEAD transcriptional complex is a promising strategy for Hippo pathway-driven cancers, but chemically tractable small-molecule chemotypes with in vivo activity remain limited. Here, we describe the optimization of a pirlindole-derived tetracyclic pyrazinocarbazole scaffold t...