Bryophytes are considered the first land plants or amphibians of the plant kingdom, with unique thallus structures with no roots and a cuticle over the thallus surface and peculiar water relations as they are considered Poikilohydric plants. These plants have proven ecological significance as water reservoirs, but economically, their worth has to be proven. Usually, sphagnum is considered an economically important plant because of its utility in various fields such as horticulture, fuel, medicine, etc. However, apart from this moss genus, only a few species have been designated with economic implications and, there are lots of species in bryophytes that have shown the presence of economically important phytoconstituents. But, generally, they are somewhat neglected for their phytochemistry and curative properties, aside from their huge diversity, second only to angiosperms. As a result of this knowledge gap about bryophytes, this study will concentrate on the valuable bioactive phytoconstituents that have been documented to date from bryophytes and have useful bioactive components. Currently, bryophytes are expected to supply a vast reservoir of new phytoconstituents for therapeutic use. The phytochemistry of various commonly occurring and easy-to-collect bryophytes has been discussed in almost complete detail in this review, along with their confirmed phytotoxic, antimicrobial, antifungal and cytotoxic properties. This effort has demonstrated that bryophytes hold tremendous promise as a source of various significant and novel bioactive compounds with medicinal and preventive functions. Researchers in bryology, phytochemistry and drug discovery will find the compilation particularly useful.