Melphalan: Recent insights on synthetic, analytical and medicinal aspects

Pahwa, Rakesh; Chhabra, Jatin; Kumar, Raj; Narang, Rakesh

doi:10.1016/j.ejmech.2022.114494

Cited by 8 publications

(1 citation statement)

References 120 publications

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“… Examples of enantiomeric pairs in the group of chiral anticancer compounds [ 43 , 44 ]. ( A ) Melphalan carrying the stereogenic centre (marked with asterix)—carbon with four different atoms or groups.…”

Section: Figurementioning

confidence: 99%

Analogues of Anticancer Natural Products: Chiral Aspects

Valentová

Lintnerová

Miklášova

et al. 2023

IJMS

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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.

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Section: Figurementioning

confidence: 99%