The heterocyclic 3H‐pyrrolo[2,3‐c]quinoline system and its closely related natural products, the marinoquinolines, have been attracting considerable attention in recent years in view of its interesting chemistry and diverse biological activities. Known since 1924, only in 2006 were the 3H‐pyrrolo[2,3‐c]quinolines associated with the first marinoquinolines isolated from natural sources. Their architecture and biological activities such as antiplasmodial, anti‐proliferative, anti‐bacterial, antifungal, phosphodiesterase and AChE inhibitors, and as ion‐sensing have stimulated the development of new strategies to obtain the natural marinoquinolines and new 3H‐pyrrolo[2,3‐c]quinoline derivatives. This review details the recent synthesis and biological evaluation of natural and unnatural marinoquinolines and its 3H‐pyrrolo[2,3‐c]quinoline core.
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