A stimuli-sensitive linker is one of the indispensable components of prodrugs for cancer therapy as it covalently binds the drug and releases it upon external stimulation at the tumour site. Quinone methide elimination has been widely used as the key transformation to release drugs based on their nucleofugacity. The usual approach is to bind the drug to the linker as a carbamate and release it as a free amine after a self-immolative 1,6-elimination.
View Article and Find Full Text PDFWe report a catalytic asymmetric protocol for the preparation of chiral pyrrolidinones proceeding via a radical pathway. The chemistry exploits the combination of photoredox catalysis and Lewis base catalysis to realise the first example of asymmetric radical conjugate addition to α,β-unsaturated anhydrides and esters. The reaction is initiated by photoredox activation of N-arylglycines to generate, upon decarboxylation, α-amino radicals.
View Article and Find Full Text PDFImprovements in cancer care over the years have increased the numbers of cancer survivors. Therefore, quality of life, fat mass management and physical activity are growing areas of interest in these people. After the surgical removal of a breast cancer, adjuvant therapy remains anyway a common strategy.
View Article and Find Full Text PDFAntitumor hydroxamates SAHA and Dacinostat have been linked to cetuximab and trastuzumab through a non-cleavable linker based on the p-mercaptobenzyl alcohol structure. These antibody drug conjugates (ADCs) were able to inhibit HDAC in several tumour cell lines. The cetuximab based ADCs block human lung adenocarcinoma cell proliferation, demonstrating that bioconjugation with antibodies is a suitable approach for targeted therapy based on hydroxamic acid-containing drugs.
View Article and Find Full Text PDFNutr Metab Cardiovasc Dis
August 2020
Background And Aims: Great attention is now being paid to effective policies and programs to promote physical activity among adolescents, girls consistently found to be less active than boys. The aim of this study was to assess gender differences in perceived barriers for physical activity practice and their relationship with physical activity levels and physical condition among adolescents.
Methods And Results: A cross-sectional study was conducted in February-April 2017 among students (n = 368) in the last year of two state high schools in Florence (Italy).
Introduction: Lifestyle factors, as eating habits and physical activity, are associated with health and productivity of workers. The aim of this study is an assessment of lifestyle of the employees of an international company of household items.
Methods: 291 (170 female, 121 male) employees underwent body composition assessment and completed two questionnaires (International Physical Activity Questionnaire and National Institute for Research of the Food and Nutrition).
Soccer referees are a specific group of the athletes' population whose careers peak from 30 to 45 years old. An athlete's performance is not only determined by physical training but also by a lifestyle, e.g.
View Article and Find Full Text PDFInt J Environ Res Public Health
December 2019
The aim of the study is to establish a simple and low-cost method that, associated with Body Mass Index (BMI), differentiates overweight conditions due to a prevalence of lean mass compared to an excess of fat mass during the evaluation of young athletes. 1046 young athletes (620 male, 426 female) aged between eight and 18 were enrolled. Body composition assessments were performed with anthropometry, circumferences, skinfold, and bioimpedance.
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