Life is chiral, as its constituents consist, to a large degree, of optically active molecules, be they macromolecules (proteins, nucleic acids) or small biomolecules. Hence, these molecules interact disparately with different enantiomers of chiral compounds, creating a preference for a particular enantiomer. This chiral discrimination is of special importance in medicinal chemistry, since many pharmacologically active compounds are used as racemates—equimolar mixtures of two enantiomers. Each of these enantiomers may express different behaviour in terms of pharmacodynamics, pharmacokinetics, and toxicity. The application of only one enantiomer may improve the bioactivity of a drug, as well as reduce the incidence and intensity of adverse effects. This is of special significance regarding the structure of natural products since the great majority of these compounds contain one or several chiral centres. In the present survey, we discuss the impact of chirality on anticancer chemotherapy and highlight the recent developments in this area. Particular attention has been given to synthetic derivatives of drugs of natural origin, as naturally occurring compounds constitute a major pool of new pharmacological leads. Studies have been selected which report the differential activity of the enantiomers or the activities of a single enantiomer and the racemate.
Many drugs are chiral and their therapeutic activity depends on specific recognition of chiral biomolecules. The biological activity of enantiomers can also differ drastically in terms of toxicity and pharmacokinetics. Chiral natural biological molecules, such as nucleic acids, enzymes are targeted molecules for the development of anticancer drugs. The interest in chiral agents is logically a result of the different interaction with biomolecules leading in the end consequence to improve anticancer activity and maybe to less undesirable effects. This review outlines the effects of chirality on the efficiency of anticancer metal-based agents and potential organic drugs. A variety of up-to-date examples of structurally diverse chiral agents exhibiting different mechanisms in their antitumor activity is presented.
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