Applications of Click Chemistry in Drug Discovery and Development

This chapter deals with 1,2,3-triazoles that are under various stages of investigation in the field of drug discovery and development. It also deals with the synthesis of 1,2,3-triazole-based drugs, which have already been in the market or have been approved. Drug discovery and development involve syntheses of new chemical entities/new molecular entities from the basic understanding of different disease processes. Synthesis of biologically active compounds possessing the 1,2,3-triazole core through 1,3-dipolar cycloaddition reactions has been reviewed. As the human carbonic anhydrase (CAs) IX and XII are validated, antitumor targets, such prodrug, isoform-selective inhibitors as the sulfocoumarins reported earlier, may be useful for identifying suitable drug candidates for clinical trials. A recent review focuses mainly on the applications of click reaction in the synthesis of agents with mechanism-based anticancer activity, which are divided into four groups: Topoisomerase II inhibitors, HDAC inhibitors, protein tyrosine kinase (PTK) inhibitors, and antimicrotubule agents.