Botanical resources have served as a cornerstone of drug discovery from ancient civilizations to modern pharmaceutical research. Plants synthesize a vast array of secondary metabolites that exhibit diverse biological activities and therapeutic potential. In recent years, the resurgence of interest in natural products has been driven by limitations of synthetic drugs, rising antimicrobial resistance and the need for safer, cost-effective therapeutics. Advances in biotechnology, omics sciences, computational tools and analytical chemistry have significantly enhanced the exploration and utilization of botanical resources. Despite these advancements, challenges such as phytochemical complexity, lack of standardization, biodiversity loss and regulatory constraints continue to hinder progress. This chapter examines the role of botanical resources in drug discovery, highlights emerging research innovations, discusses existing challenges and emphasizes the importance of multidisciplinary and sustainable approaches in translating plant-based compounds into effective medicines.