The 1,4-dihydropyridines (DHPs), a class of drugs, possess a wide variety of biological and pharmacological actions, have represented one of the most important groups of calcium-channel-modulating agents and have experienced widespread use in the treatment of cardiovascular disease. Moreover, it has been demonstrated that DHPs could prove to be highly important as multidrug-resistance-reversing agents in cancer chemotherapy. Recent reports suggest that this class also has other notable activities, particularly as antimycobacterial and anticonvulsant agents. Finally, it might be possible for the DHP motif to serve as a scaffold for other pharmacological applications.