Cancer, one of the most devastating degenerative diseases nowadays, is one of the
main targets in Medicinal Chemistry and Pharmaceutical industry. Due to the significant increase
in the incidence of cancer within world population, together with the complexity of
such disease, featured with a multifactorial nature, access to new drugs targeting different biological
targets connected to cancer is highly necessary.
Among the vast arsenal of compounds exhibiting antitumor activities, this review will cover
the use of carbohydrate derivatives as privileged scaffolds. Their hydrophilic nature, together
with their capacity of establishing selective interactions with biological receptors located on
cell surface, involved in cell-to-cell communication processes, has allowed the development
of an ample number of new templates useful in cancer treatment.
Their intrinsic water solubility has allowed their use as of pro-drug carriers for accessing
more efficiently the pharmaceutical targets. The preparation of glycoconjugates in which the
carbohydrate is tethered to a pharmacophore has also allowed a better permeation of the drug
through cellular membranes, in which selective interactions with the carbohydrate motifs are
involved. In this context, the design of multivalent structures (e.g. gold nanoparticles) has
been demonstrated to enhance crucial interactions with biological receptors like lectins, glycoproteins
that can be involved in cancer progression.
Moreover, the modification of the carbohydrate structural motif, by incorporation of metal
complexes, or by replacing their endocyclic oxygen, or carbon atoms with heteroatoms has
led to new antitumor agents.
Such diversity of sugar-based templates with relevant antitumor activity will be covered in