Coumarin enjoys an important place in
drug discovery process due to its presence in diversity of biologically active compounds. Many compounds of plant origin are derivatives of
coumarin. Taking these natural products as lead, research groups across the globe have designed and synthesized numerous
coumarin analogues for treatment of varied diseases.
Cancer is one of the dreadful
chronic diseases, and many drugs are available for its treatment. However, due to heterogeneity of
cancer, the search is still on to develop drugs for specific types of
cancers. The present review is an attempt to study various
coumarin derivatives of natural as well as synthetic origins, which are identified or developed for the treatment of different types of
cancers. Herein, we have classified various anticancer
coumarin derivatives on the basis of their origin as well as substitution around it. These are discussed under the headings of natural, semi-synthetic and synthetic
coumarin derivatives. The synthetic
coumarin derivatives are further classified as mono-, di- and poly-substituted and fused
coumarin derivatives. Of the six positions available for substituents on
coumarin nucleus, only three positions (C-3, C-4 and C-7) are exploited for the selection of functional groups appropriate for anticancer activity. The other positions (C-5, C-6 and C-8) are either unexplored or very less exploited. The present review is expected to provide the medicinal chemists a guide to choose new functional groups for substitution at different positions of
coumarin nucleus for development of novel compounds for the treatment of a specific type of
cancer.