Cancer remains the most devastating disease that threatens public health
with increasing incidence year by year worldwide. The anti-cancer property of
naturally derived compounds appears to be a promising approach in cancer therapy.
Terpenoids, generally known as terpenes, belong to the most abundant secondary
metabolites class and extensively occur in various medicinal plants, fruits, and
vegetables. Most of the terpenoids are non-toxic in nature and a ubiquitous part of the
human diet. To date, approximately 50,000 terpenoids have been known in nature, and
most of them have their use in traditional as well as modern medicinal systems. Based
on the number of cyclic structures, terpenoids have been classified into eight main
classes such as hemiterpenoids, monoterpenoids, sesquiterpenoids, diterpenoids,
sesterterpenoids, triterpenoids, tetraterpenoids, and polyterpenoids. Terpenoids have
shown several biological and pharmaceutical significances, including anticancer
activity. The literature study revealed that terpenoids exhibit anticancer activity against
various human cancers via inhibiting the initiation and progression of tumor growth in
vitro and in vivo. In addition, many terpenoids inhibit cell proliferation, invasion,
metastasis, and angiogenesis which promote apoptosis of various cancer cells via
inhibiting various deregulated oncogenic intracellular signaling pathways. Moreover,
the pre-clinical anticancer efficacy of terpenoids supports their clinical application as
an anticancer therapeutic. This chapter attempts to provide a comprehensive overview
of recent advancements and mechanistic progress on terpenoids as cancer therapeutic
Keywords: Apoptosis, Cytotoxicity, Cancer, Diterpenoids, Hemiterpenoids, Monoterpenoids, Oncogenic signaling pathways, Phytochemicals, Polyterpenoids, Sesquiterpenoids, Sesterterpenoids, Terpenoids, Triterpenoids, Tetraterpenoids.