Here, we present the current state of knowledge on the diversity of Chilean bryophytes (mosses, liverworts, and hornworts), the secondary metabolites present in these plants, and the biological activity of extracts from populations of Chilean species. Our goal is to establish the potential of these plants as a source of useful molecules for pharmaceutical and agricultural industries, thus promoting their conservation. Only 3,7% of Chilean bryophytes (55 spp.) have been analyzed using chemical characterization of their extracts (methanol, ether, ethanol, dichloromethane, acetone and hexane). Only four species from Chilean and Argentinian populations (Porella chilensis (Lehm. & Lindenb.) Trevi., Riccardia polyclada (Mitt. ex Thurn) Hassel, Balantiopsis cancellata (Nees) Stephani, and Sphagnum magellanicum Brid.) have been evaluated for biological activity. The majority of these studies have concentrated on liverworts widely distributed in the Southern Hemisphere and in the temperate forests of the southern half of Chile and adjacent Argentina. We briefly discuss aspects related to the use of bioprospecting as a conservation tool as well as the maintenance of in vitro bryophyte cultures with the goal of conservation and production.