Medicinal chemistry of natural products focuses on the discovery, design, and development of bioactive compounds derived from natural sources like plants, microbes, and marine organisms. These compounds often serve as lead structures for new drug development due to their diverse chemical scaffolds. Natural products have historically played a vital role in treating diseases such as cancer, infections, and inflammation. Advanced techniques like structure-activity relationship (SAR) studies and molecular docking are used to enhance their pharmacological profiles. Isolation and structural elucidation involve modern spectroscopic methods including NMR and MS. Synthetic modification improves efficacy, selectivity, and drug-like properties. Many FDA-approved drugs are natural product derivatives. This field bridges traditional medicine with modern drug discovery platforms.