Chromone: A Valid Scaffold in Medicinal Chemistry

Abstract

The last few decades have provided stunning progresses in the understanding of physiopathology of several diseases. The remarkable progress in research fields, like genetics, immunology, neurobiology, among others, as well as the advent of more powerful tools, have made it possible to characterize, monitor, and understand far more of the basis of physiology and disease. However, for some diseases the treatment remains a problematic issue as the efforts performed so far were not translated into therapeutic solutions. Notwithstanding the steady increase in the total amount of FCUP

An Overview of 2‐Styrylchromones: Natural Occurrence, Synthesis, Reactivity and Biological Properties

“…the A component in structure 1, Figure 1), a well-known class of oxygenated heterocyclic compounds, play an important role in nature due to their recognized biological, pharmacological and biocidal activities. [1][2][3] These effects of these naturally occurring compounds, associated with the large variety of substituents and positions in their skeleton, have resulted in strong demand over the years for their isolation in large amounts, for the development of efficient and eco-friendly routes for their synthesis, as cyclic systems and important intermediates in the search for bioactive compounds. It is our intention in this review to give a general overview on the natural occurrence, synthesis, reactivity and biological properties of 2-styrylchromones, which were published up until 2016.…”

“…Moreover, the chromone ring system is a valuable starting material in many chemical reactions leading to the preparation of a wide variety of synthetic derivatives, some of them used nowadays as therapeutic agents. [2,4] It is therefore the alliance of chemistry and biological activities that forms the basis of this review, dedicated to the versatility of a small group of chromones possessing a styryl moiety (B component in structure 1, Figure 1) at position 2 and known as 2-styrylchromones 1 [or (E)-2-styryl-4H-chromen-4-one, 2-SC, Figure 1]. Here we cover the sparse natural occurrence, synthesis, reactivity and biological profile of 2-styrylchromones in a a single and general overview intended to highlight better the importance of this small group of oxygen-containing heterocycles.…”

<strong>Ultrasound-promoted Kabachnik&ndash;Fields </strong><strong>Synthesis and Docking Studies of Novel Coupled Chromonyl-thiadiazolyl Derivatives. </strong>

“…Chromone and chromone derivatives are ubiquitous structures that constitute a variety of naturally occurring and synthetic bioactive compounds [19]. Chromones are oxygen-containing heterocycles with a benzoannelated γ-pyrone ring.…”

Quantitative Structure–Cytotoxicity Relationship of 2-(N-cyclicamino)chromone Derivatives

“…4H-1-Benzopyran-4-one (chromone) are an important class of oxygenated heterocyclic compounds, since the core structure is found ubiquitously in the plant kingdom in notable amounts (1), and thus provides a backbone structure for the synthesis of various derivatives. 2-Aminochromone derivatives showed various biological activities including anti-inflammatory activity (2,3), antimicrobial activity (3), phosphodiesterase inhibition (4,5), modulation of DNA repair (6), inhibitors of DNA-dependent protein kinase and radiosensitization of a human tumor cell line (7) and new potential PET agents for imaging of DNA-dependent protein kinase (DNA-PK) in cancer (8).…”