ABSTRACT A PPh 2 Me‐promoted 4 + 3 annulation between benzo c 1,2dithiol‐3‐ones and quinazoline‐derived azomethine imines for the facile synthesis of a novel quinazoline‐fused benzothiadiazepine library is described. This transformation is characterized by its mild conditions and excellent functional group tolerance, affording 25 novel tetracyclic compounds in excellent yields (most >85%). The biological evaluation of the obtained tetracyclic products established the scaffold's promising preliminary anti‐TNBC profile. The lead compound, 3ma , further demonstrated potent anti‐migratory effects in wound healing and transwell assay, suggesting anti‐metastatic potential. Preliminary mechanistic insights from molecular docking studies indicated binding affinity to the EGFR kinase active site, which provides a testable hypothesis for the mechanism of action.
Sun et al. (Sat,) studied this question.