Online now: Click chemistry in natural product drug discovery and development
Natural products are vital to drug discovery but are often limited by poor solubility, stability, and target specificity. Click chemistry, with its efficient and bioorthogonal reactions, enables precise modification of these compounds. It is instrumental in key discovery stages: chiral separation, high-throughput screening library construction, target identification using activity-based probes, and prodrug structural optimization. Under mild conditions, modular click reactions markedly improve the druggability of natural products. This review surveys these applications and discusses future directions, including integration with artificial intelligence, positioning click chemistry as a key platform for developing next-generation natural product-based therapeutics.
