Reversed-phase thin-layer chromatography and reversed-phase high-performance liquid chromatography were used for lipophilicity determination of a library of 30 thiazole chalcones and aurones previously synthetized in our laboratory. The experimental lipophilicity data have been compared with theoretical lipophilicity parameters estimated by various computational methods. Good correlations between the experimental and calculated lipophilicity parameters have been found for both investigated classes of compounds. Correlations between the lipophilicity of the thiazole chalcones and aurones and their antiproliferative activity were discussed. The methodologies and data gathered in this study will contribute to the lipophilicity studies of chalcones and aurones derivatives, two important classes of compounds in medicinal chemistry.
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http://dx.doi.org/10.1002/jssc.202000262 | DOI Listing |
Sci Rep
December 2024
School of Biological Engineering, Henan University of Technology, No. 100 Lianhua Street, Zhengzhou High-Tech Development Zone, Zhengzhou, 450001, Henan, People's Republic of China.
Nat Prod Res
November 2024
Graduate School of Food and Nutritional Sciences, Toyo University, Saitama, Japan.
, an annual herb belonging to the Leguminosae family, is traditionally consumed as tea in the form of dried whole herbs or beans. To deepen our understanding of the chemical constituents of we isolated 16 compounds, categorised as flavone derivatives (-), including a novel compound nomameflavone A (), a chalcone derivative (), an aurone derivative (), a chromone derivative (), a juglone derivative (), anthraquinone derivatives (-), phenolic compounds (-), and sterol derivatives (, ). The structure of each compound was elucidated using NMR and MS.
View Article and Find Full Text PDFRSC Med Chem
May 2024
Université de Franche-Comté, EFS, INSERM, UMR RIGHT F-25000 Besançon France
Arginase, a difficult-to-target metalloenzyme, is implicated in a wide range of diseases, including cancer, infectious, and cardiovascular diseases. Despite the medical need, existing inhibitors have limited structural diversity, consisting predominantly of amino acids and their derivatives. The search for innovative arginase inhibitors has now extended to screening approaches.
View Article and Find Full Text PDFBioorg Med Chem Lett
January 2024
Faculty of Pharmacy, University of Medicine and Pharmacy at Ho Chi Minh City, Ho Chi Minh City 700000, Viet Nam.
Aurones are a minor subgroup of flavonoids. Unlike other subgroups such as chalcones, flavones, and isoflavones, aurones have not been extensively explored as pancreatic lipase inhibitors. In this work, we studied the pancreatic lipase inhibitory potency of synthetic aurone derivatives.
View Article and Find Full Text PDFJ Ethnopharmacol
March 2024
Department of Botany, Universidade Federal de Pernambuco - UFPE, Rua Professor Moraes Rego, s/n, Recife, Pernambuco, 50.670-901, Brazil.
Ethnopharmacological Relevance: Hancornia speciosa Gomes is a fruit and medicinal species used for treating infectious diseases of the genitourinary system. However, its mechanism of action against microbes is still not fully understood. Infections in the genitourinary system caused by Candida spp.
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