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Molecules 2019, 24(1), 180; https://doi.org/10.3390/molecules24010180

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

1
Laboratório de Química Orgânica e Farmacêutica, Departamento de Ciências Químicas, Faculdade de Farmácia, Rua de Jorge Viterbo Ferreira, 228, 4050-313 Porto, Portugal
2
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
3
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
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Abstract

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
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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.

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