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1.
Chem Rec ; 24(2): e202300221, 2024 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-37594737

RESUMEN

The literature on cyclic sulfinamides (put simply, sultims) published from 1989 to 2022 has been summarized and reviewed. The information is divided into two sections: the analysis of synthetic methods on the preparation of cyclic sulfinamides and the discussion of the chemical properties of cyclic sulfinamides focusing on their reactions and applications. The survey of the reaction conditions, provided in the most detailed way, and a critical view of the reaction mechanisms add an extra dimension to the text. The data presented will be useful to specialists in different areas, especially those who work in the field of synthetic organic and pharmaceutical chemistry.

2.
Mini Rev Med Chem ; 20(2): 107-122, 2020.
Artículo en Inglés | MEDLINE | ID: mdl-31595850

RESUMEN

Quercetin is a plant flavonoid with great potential for the prevention and treatment of disease. Despite the curative application of quercetin is hampered by low bioavailability, its core serves as a scaffold for generating more potent compounds with amplified therapeutic window. This review aims to describe recent advances in the improvement of the pharmacokinetic profile of quercetin via the amino acid prodrug approach which offers wide structural diversity, physicochemical and biological properties improvement. According to the findings, conjugation of quercetin with amino acids results in increased solubility, stability, cellular permeability as well as biological activity. In particular quercetin- amino acid conjugates exhibited potent anticancer, MDR-reversal and antibiotic resistance reversal activities. The synthetic pathways and examples of quercetin-amino acid conjugates are considered. Practical considerations and challenges associated with the development of these prodrugs are also discussed. This mini-review covers the literature on quercetin-amino acid conjugates since 2001 when the first thematic work was published.


Asunto(s)
Aminoácidos/farmacología , Antineoplásicos/farmacología , Descubrimiento de Drogas , Neoplasias/tratamiento farmacológico , Profármacos/farmacología , Quercetina/farmacología , Aminoácidos/química , Animales , Antineoplásicos/química , Apoptosis/efectos de los fármacos , Proliferación Celular/efectos de los fármacos , Humanos , Estructura Molecular , Neoplasias/patología , Profármacos/química , Quercetina/química
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