Natural products constitute an important source for drug discovery to improve human health. At the present time, novel structures of natural products are difficult to isolate from specimens grown under normal conditions. Taking advantage of the genomic, metabolomic, and proteomic databases, the new natural product sciences emerged in the late 20th century. These efforts have resulted in finding novel bioactive natural products. In parallel, robust assay methods to screen natural product libraries and structure-based drug design has proven to be progressable tactics in modern drug discovery programs. The aim of this special issue seeks original research articles and reviews on bioactive natural products, natural product-based medicinal chemistry, chemical syntheses of bioactive natural products, new assay methods to screen natural products, computational chemistry to improve efficacy of natural products, pharmacokinetic and dynamic aspects of drugs of natural product origin, and new strategy to use approved natural product derivatives.

Keywords: Bioactive natural products, assay-guided isolations, genome mining, synthesis, medicinal chemistry, biosynthesis, proteomics, drug targets