Bioactive compounds are natural compounds obtained from plants that have specific therapeutic or health benefits. These compounds have specific properties including antioxidant, anti-inflammatory, antidiabetic, anticancer, and antimicrobial properties which contribute to their biologically active nature apart from their nutritive value. On the basis of their chemistry, these bioactive compounds comprise different classes like flavonoids, anthocyanins, tannins, betalains, carotenoids, plant sterols, and glucosinolates. These compounds due to their incomparable properties facilitate pivotal roles in different biological processes, including cellular signalling, metabolism, and defense mechanisms. Understanding their mechanisms of action and physiological effects is crucial for harnessing their potential in pharmaceuticals, nutraceuticals, and functional foods. Numerous researches have focused on developing extraction techniques of bioactive compounds from plant sources for a wide range of applications. Several conventional extraction techniques are Soxhlet extraction, maceration, hydro-distillation, infusion, and decoction while non-conventional extraction techniques are pulsed electric field extraction, enzyme-assisted extraction, microwave-assisted extraction, supercritical fluid extraction, ultrasound-assisted extraction and pressurized liquid extraction. This chapter provides a comprehensive view of the fundamentals of bioactive compounds, their classification, extraction techniques, and applications highlighting their significance in health, medicine, and biotechnology.