Next Article in Journal
Cardiomyocyte Progenitor Cells as a Functional Gene Delivery Vehicle for Long-Term Biological Pacing
Next Article in Special Issue
Structures, Activities and Drug-Likeness of Anti-Infective Xanthone Derivatives Isolated from the Marine Environment: A Review
Previous Article in Journal
Solid-Phase Synthesis and Circular Dichroism Study of β-ABpeptoids
Previous Article in Special Issue
New Alkoxy Flavone Derivatives Targeting Caspases: Synthesis and Antitumor Activity Evaluation
Article Menu
Issue 1 (January-1) cover image

Export Article

Open AccessFeature PaperReview
Molecules 2019, 24(1), 180;

Carboxyxanthones: Bioactive Agents and Molecular Scaffold for Synthesis of Analogues and Derivatives

Laboratório de Química Orgânica e Farmacêutica, Departamento de Ciências Químicas, Faculdade de Farmácia, 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.
Academic Editors: Maria Emília de Sousa, Honorina Cidade and Carlos Manuel Afonso
Received: 19 December 2018 / Revised: 31 December 2018 / Accepted: 2 January 2019 / Published: 5 January 2019
PDF [3439 KB, uploaded 5 January 2019]


Xanthones represent a structurally diverse group of compounds with a broad range of biological and pharmacological activities, depending on the nature and position of various substituents in the dibenzo-γ-pyrone scaffold. Among the large number of natural and synthetic xanthone derivatives, carboxyxanthones are very interesting bioactive compounds as well as important chemical substrates for molecular modifications to obtain new derivatives. A remarkable example is 5,6-dimethylxanthone-4-acetic acid (DMXAA), a simple carboxyxanthone derivative, originally developed as an anti-tumor agent and the first of its class to enter phase III clinical trials. From DMXAA new bioactive analogues and derivatives were also described. In this review, a literature survey covering the report on carboxyxanthone derivatives is presented, emphasizing their biological activities as well as their application as suitable building blocks to obtain new bioactive derivatives. The data assembled in this review intends to highlight the therapeutic potential of carboxyxanthone derivatives and guide the design for new bioactive xanthone derivatives. View Full-Text
Keywords: xanthone scaffold; carboxyxanthone derivatives; carboxyxanthone analogues; bioactivities xanthone scaffold; carboxyxanthone derivatives; carboxyxanthone analogues; bioactivities

Figure 1

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

Ribeiro, J.; Veloso, C.; Fernandes, C.; Tiritan, M.E.; Pinto, M.M.M. Carboxyxanthones: Bioactive Agents and Molecular Scaffold for Synthesis of Analogues and Derivatives. Molecules 2019, 24, 180.

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