Recent insight into the biological activities of synthetic xanthone derivatives

Shagufta,; Ahmad, Irshad

doi:10.1016/j.ejmech.2016.03.058

Cited by 146 publications

(71 citation statements)

References 92 publications

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“…Thus,currently, the development of xanthone as anti MRSA is more directed to design and development of smaller molecules with higher membran selectivity to lessen the toxicity against normal mamalian cells. 49 Some efforts that has already been done is adding a lipophylic functional groups, like those in xanthone amphiphilic compound, which produce higher anti MRSA activity with lower membrane selectivity and lower toxicity.…”

Section: The Antibacterial Mechanism Of Xanthone Compounds Against Mrsamentioning

confidence: 99%

Potency of Xanthone Derivatives as antibacterial agent against Methicillin-Resistant Staphylococcus Aureus (MRSA)

Miladiyah

Rachmawaty

2017

JKKI

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Section: The Antibacterial Mechanism Of Xanthone Compounds Against Mrsamentioning

confidence: 99%

Potency of Xanthone Derivatives as antibacterial agent against Methicillin-Resistant Staphylococcus Aureus (MRSA)

Miladiyah

Rachmawaty

2017

JKKI

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“…Moreover, enantioselectivity for HSA binding has been reported for several drugs such as verapamil and ibuprofen [18], being also predicted by docking studies [19,20]. One group of compounds described with antitumor [21,22,23], anti-inflammatory [24,25,26], among others activities [27,28], concerns xanthone derivatives. Indeed, the xanthone scaffold can be considered a privileged structure [28].…”

Section: Introductionmentioning

confidence: 98%

Chiral Derivatives of Xanthones: Investigation of the Effect of Enantioselectivity on Inhibition of Cyclooxygenases (COX-1 and COX-2) and Binding Interaction with Human Serum Albumin

et al. 2017

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Searching of new enantiomerically pure chiral derivatives of xanthones (CDXs) with potential pharmacological properties, particularly those with anti-inflammatory activity, has remained an area of interest of our group. Herein, we describe in silico studies and in vitro inhibitory assays of cyclooxygenases (COX-1 and COX-2) for different enantiomeric pairs of CDXs. The evaluation of the inhibitory activities was performed by using the COX Inhibitor Screening Assay Kit. Docking simulations between the small molecules (CDXs; known ligands and decoys) and the enzyme targets were undertaken with AutoDock Vina embedded in PyRx—Virtual Screening Tool software. All the CDXs evaluated exhibited COX-1 and COX-2 inhibition potential as predicted. Considering that the (S)-(−)-enantiomer of the nonsteroidal anti-inflammatory drug ketoprofen preferentially binds to albumin, resulting in lower free plasma concentration than (R)-(+)-enantiomer, protein binding affinity for CDXs was also evaluated by spectrofluorimetry as well as in in silico. For some CDXs enantioselectivity was observed.

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“…Xanthones are called ‘promiscuous binders’ because of their capacity to bind to different receptors, exerting pronounced pharmacological activity against several diseases . Therefore, organic chemists have also focused on the study of synthetic xanthone derivatives, aiming at the development of new drug candidates with anti‐inflammatory, antioxidant, and anticancer properties, among others …”

Section: Introductionmentioning

confidence: 99%

“…Because of their great importance in the field of natural products, xanthones have already been reviewed several times in the literature . Recently, our research group highlighted xanthones as a promising source of anticancer compounds with oral bioavailability .…”

Section: Introductionmentioning

confidence: 99%

Xanthones and Cancer: from Natural Sources to Mechanisms of Action

Klein‐Júnior

Campos

Niero

et al. 2020

Chemistry & Biodiversity

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Xanthones are a class of heterocyclic natural products that have been widely studied for their pharmacological potential. In fact, they have been serving as scaffolds for the design of derivatives focusing on drug development. One of the main study targets of xanthones is their anticancer activity. Several compounds belonging to this class have already demonstrated cytotoxic and antitumor effects, making it a promising group for further exploration. This review therefore focuses on recently published studies, emphasizing their natural and synthetic sources and describing the main mechanisms of action responsible for the anticancer effect of promising xanthones.

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Recent insight into the biological activities of synthetic xanthone derivatives

Cited by 146 publications

References 92 publications

Potency of Xanthone Derivatives as antibacterial agent against Methicillin-Resistant Staphylococcus Aureus (MRSA)

Potency of Xanthone Derivatives as antibacterial agent against Methicillin-Resistant Staphylococcus Aureus (MRSA)

Chiral Derivatives of Xanthones: Investigation of the Effect of Enantioselectivity on Inhibition of Cyclooxygenases (COX-1 and COX-2) and Binding Interaction with Human Serum Albumin

Xanthones and Cancer: from Natural Sources to Mechanisms of Action

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