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1.
Chem Commun (Camb) ; 60(4): 436-439, 2024 Jan 04.
Artículo en Inglés | MEDLINE | ID: mdl-38086706

RESUMEN

Sulf-2 has been identified as a putative target for anticancer therapies. Here we report the design and synthesis of sulfated disaccharide inhibitors based on IdoA(2S)-GlcNS(6S). Trisulfated disaccharide inhibitor IdoA(2S)-GlcNS(6Sulfamate) demonstrated potent Sulf-2 inhibition. The IC50 value was determined to be 39.8 µM ± 18.3, which is comparable to a tetrasaccharide inhibitor of HSulf-1 reported in the literature. We propose that the disaccharide IdoA(2S)-GlcNS(6S) is the shortest fragment size required for effective inhibition of the Sulfs.


Asunto(s)
Heparitina Sulfato , Oligosacáridos , Heparitina Sulfato/farmacología , Oligosacáridos/farmacología , Disacáridos/farmacología , Sulfotransferasas
2.
Stud Health Technol Inform ; 289: 309-312, 2022 Jan 14.
Artículo en Inglés | MEDLINE | ID: mdl-35062154

RESUMEN

AIM: Feasibility-reliability control of Telemedicine Systems (TS) integrated with Multimedia Systems (MS) and Artificial intelligence (AI) for remote e-Multidisciplinary Oncology Conference in Breast Cancer. MATERIAL AND METHODS: Forty (n1=40) patients suffering from breast surgical oncology malignant (n2=32) and non-malignant (n3=8) diseases classified to seven categories: Nipple Discharge, Dominant Breast Mass, Occult Breast Lesion, Early Breast Carcinoma, Advanced Breast Carcinoma, Recurrent Breast Carcinoma) and treated clinically with the standard diagnostic (Mammography, US, MRI, Cytology, Pathology, BRCA1/2 Mutation Predisposition and Breast Cancer Risk Analysis) surgical, auxiliary therapeutic methods. Then clinical decisions compared to those proposed remotely by the virtual AI supported e-Oncology Conference for each patient. RESULTS: In four (n4=4) out of forty patients (TS, MS and AI) supported decision making and surgical treatment proposal including postoperative Radiotherapy proposal was not as clear as expected. Non-output answer for non-malignant breast pathologies (n3=8) was accurately indicated by (MS and AI). Mean accuracy of (TS, MS and AI) for: 1.Surgical Operative Planning including Rad=94.1%, 2.Chem=96.8%, 3.Horm=96.7% [In 95%, (Confidence interval: 85-99%)]. CONCLUSION: High feasibility-reliability of the virtual AI supported e-Multidisciplinary Oncology Conference for remote decision making and surgical planning and for optimum outcomes in Breast Cancer treatment makes it a clinical necessity especially for the periphery of Hellas.


Asunto(s)
Neoplasias de la Mama , Inteligencia Artificial , Neoplasias de la Mama/terapia , Femenino , Humanos , Recurrencia Local de Neoplasia , Reproducibilidad de los Resultados , Tecnología
3.
Molecules ; 26(21)2021 Nov 02.
Artículo en Inglés | MEDLINE | ID: mdl-34771052

RESUMEN

Acute myeloid leukemia (AML) is the most aggressive type of blood cancer, and there is a continued need for new treatments that are well tolerated and improve long-term survival rates in patients. Induction of differentiation has emerged as a promising alternative to conventional cytotoxic chemotherapy, but known agents lack efficacy in genetically distinct patient populations. Previously, we established a phenotypic screen to identify small molecules that could stimulate differentiation in a range of AML cell lines. Utilising this strategy, a 1,5-dihydrobenzo[e][1,4]oxazepin-2(3H)-one hit compound was identified. Herein, we report the hit validation in vitro, structure-activity relationship (SAR) studies and the pharmacokinetic profiles for selected compounds.


Asunto(s)
Antineoplásicos/química , Antineoplásicos/farmacología , Diferenciación Celular/efectos de los fármacos , Antineoplásicos/síntesis química , Línea Celular Tumoral , Células Cultivadas , Técnicas de Química Sintética , Relación Dosis-Respuesta a Droga , Ensayos de Selección de Medicamentos Antitumorales , Humanos , Leucemia Mieloide Aguda , Estructura Molecular , Relación Estructura-Actividad
4.
Surg Today ; 41(4): 537-41, 2011 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-21431488

RESUMEN

Intracystic papillary carcinoma of the male breast represents an extremely rare entity that accounts for less than 1% of all malignancies, and histologically may range from papillary hyperplasia in gynecomastia to invasive papillary carcinoma. This report presents the case of a 61-year-old Caucasian man who presented with a 5-year history of a centrally located painless swelling of his right breast with occasional nipple discharge. Triple assessment was very helpful in establishing the diagnosis. Treatment included a mastectomy and hormonal therapy because the neoplasm expressed hormone receptors. Although male breast carcinomas tend to behave more aggressively than their female counterparts, the prognosis of this neoplasm is excellent.


Asunto(s)
Neoplasias de la Mama Masculina/diagnóstico , Carcinoma Papilar/diagnóstico , Neoplasias de la Mama Masculina/tratamiento farmacológico , Neoplasias de la Mama Masculina/patología , Neoplasias de la Mama Masculina/cirugía , Carcinoma Papilar/tratamiento farmacológico , Carcinoma Papilar/patología , Carcinoma Papilar/cirugía , Diagnóstico Diferencial , Diagnóstico por Imagen , Humanos , Escisión del Ganglio Linfático , Masculino , Mastectomía , Persona de Mediana Edad
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