Next Article in Journal
Increased Selectivity of Novozym 435 in the Asymmetric Hydrolysis of a Substrate with High Hydrophobicity Through the Use of Deep Eutectic Solvents and High Substrate Concentrations
Next Article in Special Issue
New Brush-Type Chiral Stationary Phases for Enantioseparation of Pharmaceutical Drugs
Previous Article in Journal
A Validated HPLC-MS/MS Assay for 14-O-[(4,6-Diaminopyrimidine-2-yl)thioacetyl] Mutilin in Biological Samples and Its Pharmacokinetic, Distribution and Excretion via Urine and Feces in Rats
Previous Article in Special Issue
Stereoselective Multicomponent Reactions in the Synthesis or Transformations of Epoxides and Aziridines
Article Menu
Issue 4 (February-2) cover image

Export Article

Open AccessFeature PaperReview
Molecules 2019, 24(4), 791;

Synthetic Chiral Derivatives of Xanthones: Biological Activities and Enantioselectivity Studies

Laboratório de Química Orgânica e Farmacêutica, Departamento de Ciências Químicas, Faculdade de Farmácia, Universidade do Porto, Rua de Jorge Viterbo Ferreira, 228, 4050-313 Porto, Portugal
Interdisciplinary Centre of Marine and Environmental Research (CIIMAR), Edifício do Terminal de Cruzeiros do Porto de Leixões, Av. General Norton de Matos s/n, 4050-208 Matosinhos, Portugal
Cooperativa de Ensino Superior, Politécnico e Universitário (CESPU), Instituto de Investigação e Formação Avançada em Ciências e Tecnologias da Saúde (IINFACTS), Rua Central de Gandra, 1317, 4585-116 Gandra PRD, Portugal
Authors to whom correspondence should be addressed.
These authors contributed equally to this work.
Academic Editor: Maurizio Benaglia
Received: 1 February 2019 / Revised: 17 February 2019 / Accepted: 19 February 2019 / Published: 22 February 2019
Full-Text   |   PDF [8339 KB, uploaded 22 February 2019]   |  


Many naturally occurring xanthones are chiral and present a wide range of biological and pharmacological activities. Some of them have been exhaustively studied and subsequently, obtained by synthesis. In order to obtain libraries of compounds for structure activity relationship (SAR) studies as well as to improve the biological activity, new bioactive analogues and derivatives inspired in natural prototypes were synthetized. Bioactive natural xanthones compromise a large structural multiplicity of compounds, including a diversity of chiral derivatives. Thus, recently an exponential interest in synthetic chiral derivatives of xanthones (CDXs) has been witnessed. The synthetic methodologies can afford structures that otherwise could not be reached within the natural products for biological activity and SAR studies. Another reason that justifies this trend is that both enantiomers can be obtained by using appropriate synthetic pathways, allowing the possibility to perform enantioselectivity studies. In this work, a literature review of synthetic CDXs is presented. The structures, the approaches used for their synthesis and the biological activities are described, emphasizing the enantioselectivity studies. View Full-Text
Keywords: synthetic xanthones; chiral derivatives of xanthones; bioactivities; enantioselectivity; enantiomeric purity synthetic xanthones; chiral derivatives of xanthones; bioactivities; enantioselectivity; enantiomeric purity

Graphical abstract

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

Share & Cite This Article

MDPI and ACS Style

Fernandes, C.; Carraro, M.L.; Ribeiro, J.; Araújo, J.; Tiritan, M.E.; Pinto, M.M.M. Synthetic Chiral Derivatives of Xanthones: Biological Activities and Enantioselectivity Studies. Molecules 2019, 24, 791.

Show more citation formats Show less citations formats

Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Related Articles

Article Metrics

Article Access Statistics



[Return to top]
Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top