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.
Highlights
Xanthones (9H-xanthen-9-ones) are an important class of oxygenated three-membered heterocyclic compounds with a dibenzo-γ-pyrone scaffold (1, Figure 1) [1]
This review aims to describe the research findings on biological and pharmacological activities of of natural synthetic carboxyxanthone derivatives
In 2005, two more caged carboxylated scortechinones were isolated from the fruits of Garcinia scortechinii, scortechinones R (89) and S (90), (Figure 6) [86]
Summary
Xanthones (9H-xanthen-9-ones) are an important class of oxygenated three-membered heterocyclic compounds with a dibenzo-γ-pyrone scaffold (1, Figure 1) [1]. Naturally-occurring xanthones can be found as secondary metabolites in diverse terrestrial sources including higher plants, fungi, lichens [8,9] as well as isolated from marine invertebrates, such as sponges, tunicates, mollusks and bryozoans, in addition to algae and marine microorganisms (cyanobacteria and fungi) [10,11] They comprise a variety of different types of substituents in certain positions of the xanthone scaffold, leading to a vast diversity of biological/pharmacological. This review aims to describe the research findings on biological and pharmacological activities of of natural synthetic carboxyxanthone derivatives. Their applications aschemical suitablesubstrates chemical natural and and synthetic carboxyxanthone derivatives.
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