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This mini-review provides a concise overview of the biosynthetic pathway and pharmacology of bisbenzylisoquinoline alkaloid (bisBIA) natural products. Additional emphasis is given to the methodologies in the total syntheses of both simpler acyclic diaryl ether dimers and their macrocyclic counterparts bearing two diaryl ether linkages.

Graphical abstract: The biology and total syntheses of bisbenzylisoquinoline alkaloids

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