Acquired immunodeficiency syndrome (AIDS) caused by the human immunodeficiency virus (HIV) continues to be a worldwide public health problem. However, current drugs used to treat HIV cannot completely eradicate the infection and have a series of side effects and toxicities. Therefore, it is essential to develop new anti-HIV drugs with diverse structures and novel mechanisms of action to treat HIV/AIDS. Natural products serve as a vast source of drugs and therapeutic agents, and some diterpenoid compounds have shown potential as pharmaceutical precursors to treat HIV. In the diterpenoid family, tiglianes have attracted much attention because of their complex structures and strong anti-HIV activity for drug discovery. This chapter discusses 310 tiglianes reported during 1967–2022. This chapter includes the mechanisms of action of tiglianes against HIV and discusses the anti-HIV structure–activity relationship of certain tiglianes.
Privileged Scaffolds in Drug Discovery, 2023, Pages 565-585,