ABSTRACT
The recent revolution in drug discovery technologies has important consequences for drug delivery and targeting. Traditionally new chemical entities have been identified by the screening of natural products and chemical libraries to identify potential lead compounds. These lead compounds have then been optimized through an iterative lead-optimization process involving the synthesis of analogs, the development of quantitative-structure-activity relationships and the use of molecular modeling to obtain new chemical entities with high specificity and affinity for the therapeutic target for pharmaceutical development. The development of combinatorial chemistry has led to the ability to produce vast libraries of compounds for initial screening. The evaluation of combinatorial libraries using high-throughput screening technologies allows the rapid screening of potential lead compounds with a wider molecular diversity against a broad range of therapeutic targets.
