Tetrazoles: Structure and Activity Relationship as Anticancer Agents

Heterocyclic compounds play an important role in drug design and discovery, and they have been used to treat a variety of diseases, including cancer. Cancer is one of the leading causes of death in the world. However, various drugs and therapies are available on the market. The novel synthetic drugs show promising invitro activity, but the route to clinical trials is hampered by their low bioavailability and rapid metabolism. Tetrazoles have gained a lot of attention in recent years because they have the broadest biological activity spectrum of any heterocycle. Tetrazoles are a type of nitrogen heterocycle that has been found to be active in a variety of natural products as well as the biologically active nucleus. A vast number of studies have demonstrated the importance of this moiety in medicinal chemistry. The tetrazole ring has a similar structure to carboxylic acids and functions as a bioisostere analogue. A bioisostere is a group of molecules that have similar physiological properties, including biological activity. Tetrazole derivatives have been shown to have anti-hypertension, anti-fungal, anti-malarial, anti-leishmaniasis, anti-diabetic, anti-cancer, and a variety of other biological activities. The tetrazole moiety functions as a good pharmacophore in the drug design and discovery fields, particularly in terms of rational drug design with high efficiency with structure and anti-cancer activity.

Keywords: Bioavailability, Bioisosteres, SAR, Synthesis, Tetrazole