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This review paper provides an extensive analysis of the synthesis, characterization, and multifaceted biological applications of metal complexes and nanocomposites derived from a diverse array of biopolymeric ligands. These ligands, including chitosan, 2-hydroxybenzaldehyde, and 4-aminopyridine imine, among others, have shown remarkable potential due to their biocompatibility, biodegradability, and functional versatility. The review delves into various synthetic strategies, including conventional and green synthesis approaches, and highlights advanced characterization techniques such as spectroscopy, microscopy, thermal analysis, and X-ray diffraction. Emphasizing the broad spectrum of biological activities exhibited by these compounds, the review covers antimicrobial, anticancer, antioxidant, enzyme inhibition, and drug delivery applications. By synthesizing current research and identifying key challenges and future directions, this review aims to provide valuable insights for researchers in medicinal chemistry, materials science, biotechnology, and related fields.