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1.
Explor Target Antitumor Ther ; 4(3): 498-510, 2023.
Artículo en Inglés | MEDLINE | ID: mdl-37455823

RESUMEN

Soft tissue sarcomas (STSs) are rare, heterogeneous, and very often asymptomatic diseases. Their diagnosis is fundamental, as is the identification of the degree of malignancy, which may be high, medium, or low. The Italian Medical Oncology Association and European Society of Medical Oncology (ESMO) guidelines recommend magnetic resonance imaging (MRI) because the clinical examination is typically ineffective. The diagnosis of these rare diseases with artificial intelligence (AI) techniques presents reduced datasets and therefore less robust methods. However, the combination of AI techniques with radiomics may be a new angle in diagnosing rare diseases such as STSs. Results obtained are promising within the literature, not only for the performance but also for the explicability of the data. In fact, one can make tumor classification, site localization, and prediction of the risk of developing metastasis. Thanks to the synergy between computer scientists and radiologists, linking numerical features to radiological evidence with excellent performance could be a new step forward for the diagnosis of rare diseases.

2.
Bioorg Med Chem ; 21(7): 1834-43, 2013 Apr 01.
Artículo en Inglés | MEDLINE | ID: mdl-23434134

RESUMEN

Wound healing is a significant concern in many pathologies (post-surgeries, burns, scars) and the search for new chemical entities is advisable. The lichen compound (+)-usnic acid (1) has found application in dermatological and cosmetic preparations, due to its bacteriostatic and antioxidant activities. The compound has also been shown to stimulate the wound closure of keratinocyte monolayers at subtoxic doses. Here we describe the design and synthesis of usnic acid enamines (compounds 2-11), obtained through nucleophilic attack of amino acids or decarboxyamino acids at the acyl carbonyl of the enolized 1,3 diketone. The wound repair properties of these derivatives were evaluated using in vitro and in vivo assays. Compounds 8 and 9 combine low cytotoxicity with high wound healing performance, suggesting their possible use in wound healing-promoting or antiage skin preparations.


Asunto(s)
Antiinfecciosos/química , Antiinfecciosos/uso terapéutico , Benzofuranos/química , Benzofuranos/uso terapéutico , Líquenes/química , Cicatrización de Heridas/efectos de los fármacos , Animales , Antiinfecciosos/toxicidad , Antioxidantes/química , Antioxidantes/uso terapéutico , Antioxidantes/toxicidad , Benzofuranos/toxicidad , Línea Celular , Supervivencia Celular/efectos de los fármacos , Humanos , Queratinocitos/citología , Queratinocitos/efectos de los fármacos , Masculino , Ratones , Ratas , Ratas Sprague-Dawley
3.
ChemMedChem ; 8(2): 221-5, 2013 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-23307699

RESUMEN

Au naturel! (+)-Usnic acid (green) is a weak antimalarial agent, however, in conjugation with known antimalarial scaffolds and drugs, such as dihydroartemisinin (blue), potent activity against the blood-stage parasite can be seen both in vitro and in vivo. The compound shown exhibits an IC(50) value of 1.4 nM against Plasmodium falciparum in vitro and proved nearly as efficacious as artesunate in a mouse model of infection.


Asunto(s)
Antimaláricos/química , Antimaláricos/uso terapéutico , Benzofuranos/química , Benzofuranos/uso terapéutico , Malaria Falciparum/tratamiento farmacológico , Plasmodium falciparum/efectos de los fármacos , Animales , Antimaláricos/síntesis química , Artemisininas/síntesis química , Artemisininas/química , Artemisininas/uso terapéutico , Benzofuranos/síntesis química , Productos Biológicos/síntesis química , Productos Biológicos/química , Productos Biológicos/uso terapéutico , Línea Celular , Descubrimiento de Drogas , Femenino , Malaria Falciparum/parasitología , Ratones , Pruebas de Sensibilidad Parasitaria , Ratas
4.
Mol Divers ; 15(2): 347-60, 2011 May.
Artículo en Inglés | MEDLINE | ID: mdl-21076980

RESUMEN

In this article, we describe the design, synthesis and activity evaluation of glycomimetic DC-SIGN antagonists, that use a mannose residue to anchor to the protein carbohydrate recognition domain (CRD). The molecules were designed from the structure of the known pseudo-mannobioside antagonist 1, by including additional hydrophobic groups, which were expected to engage lipophilic areas of DC-SIGN CRD. The results demonstrate that the synthesized compounds potently inhibit DC-SIGN-mediated adhesion to mannan coated plates. Additionally, in silico docking studies were performed to rationalize the results and to suggest further optimization.


Asunto(s)
Moléculas de Adhesión Celular/antagonistas & inhibidores , Diseño de Fármacos , Lectinas Tipo C/antagonistas & inhibidores , Manosa , Receptores de Superficie Celular/antagonistas & inhibidores , Bioensayo , Manosa/química , Modelos Moleculares , Unión Proteica/fisiología , Reproducibilidad de los Resultados , Relación Estructura-Actividad
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