Radiosynthesis of microtubule‐targeted theranostic methyl N‐[5‐(3’‐radiohalobenzoyl)‐1H‐benzimidazol‐2‐yl]carbamates

Microtubules are a target for a broad spectrum of drugs used as chemotherapeutics to treat hematological malignancies and solid tumors. Most of these drugs have significant dose‐limiting toxicities including peripheral neuropathies that can be debilitating and permanent. In an ongoing effort to develop safer and more effective drugs, benzimidazole‐based compounds are being developed as replacement for vincristine and similar agents. In this report, we describe radiosyntheses of novel microtubule‐targeting methyl N‐[5‐(3’‐radiohalobenzoyl)‐1H‐benzimidazol‐2‐yl]carbamates 4 that are intended as potential imaging agents and molecular radiotherapeutics. ¹²⁵I‐ and ¹³¹I‐radiolabeled derivatives were prepared either by direct radioiodination of methyl N‐(6‐benzoyl‐1H‐benzimidazol‐2‐yl)carbamate 1 or radioiododestannylation of the corresponding stannane precursor 3 . The direct radioiodination was conducted in a solution of 1 in triflic acid and produced after ~1 hour at elevated temperatures and HPLC purification on average 62% of the no‐carrier added products ¹²⁵I‐ 4 and ¹³¹I‐ 4 . Radioiododestannylation of 3’‐trimethylstannane 3 proceeded with ease at room temperature in the presence of H₂O₂ as the oxidant and produced no‐carrier‐added ¹²⁵I‐ 4 and ¹³¹I‐ 4 in high isolated yields, on average 85%. The radiohalodestannylation protocol is universal and can be applied to other radiohalides including ¹²⁴I to produce ¹²⁴I‐ 4 , a positron emission tomography agent, and ²¹¹At to produce ²¹¹At‐ 4 , an α‐particle emitting radiotherapeutic.     

Medizinstudierendenauswahl in Deutschland

Bundesgesundheitsblatt - Gesundheitsforschung - Gesundheitsschutz - Das Bundesverfassungsgericht überprüft aktuell, ob das Vergabeverfahren der Medizinstudienplätze mit dem...     

Das weltweite Medizinernetzwerk Aufklärung gegen Tabak – Ehrenamtliche Prävention made in Germany

Smoking is the leading preventable cause of premature death in Germany. The network “Education Against Tobacco” (EAT) is an initiative that was founded in Germany in 2012, in which more than 3500 medical students and physicians engage in volunteer work in about 80 medical faculties in 14 countries. In this article, the concept, activities, objectives and associated research studies oft he EAT initiative are introduced.On the school level, the initiative addresses 10- to 15-year-old secondary school students. In addition to a multimodal approach, school visits use modern media such as facemorphing apps, which are not only used by students (45,000 per year in 14 countries), but by a total of over 500,000 other people as well. The effectiveness of the school-based intervention is currently being investigated in randomised long-term studies with 20,000 adolescents in Germany. A first long-term study demonstrated evidence of a protective effect regarding the onset of smoking, especially among female students, students having a low level of education and students with a migratory background.The programme educates several hundred prospective physicians at 13 (of 28 participating) German medical faculties each year in science-based elective courses for the well-established smoking cessation counselling of patients and sensitises them to the tobacco epidemic. The approved members engage in dialogue with local members of the German house of representatives as “Ärzteverband Tabakprävention”.EAT motivates the prospective generation of physicians, initially through prevention in school settings, to face the challenge of national tobacco control at the university and federal level.     

Empowering senior citizens for healthy nutrition in Germany: A pilot study

Main goal of this study was to analyse how empowerment processes and bottom‐up activities aimed at healthier food choices and food environment could be initiated among a group of senior citizens (between 60 and 75 years old). The intervention was set up as a pilot study in a rural community (15,000 inhabitants) in the federal state of Bavaria, South Eastern Germany. A process evaluation documented how group formation and empowerment processes developed during the course of the intervention. Extensive field notes were taken in 27 meetings, interviews (n = 13) and focus groups (n = 4) were conducted with participants and key persons at different points of the intervention. Data were analysed using content analysis. The intervention succeeded in motivating senior citizens to participate in regular meetings over 11 months. During the intervention, the group members’ awareness of factors influencing their eating behaviour increased. Furthermore, they developed ideas to improve the community's food environment and accomplished duties needed to implement these ideas. However, initiating empowerment processes, especially in terms of fostering leadership and transferring responsibility, took longer than expected and could be realised only partially. The findings support a further use and evaluation of the empowerment approach for addressing nutritional aspects among senior citizens.     

Comparison of Longitudinal and Apical Foetal Speckle Tracking Echocardiography Using Tissue Motion Annular Displacement and Segmental Longitudinal Strain

The aim of our prospective pilot study with exploratory analysis was to compare longitudinal and apical foetal speckle tracking echocardiography (STE) using tissue motion annular displacement (TMAD) and segmental longitudinal strain (SLS). We compared two different STE quantification tools in a longitudinal and apical four-chamber view in 57 normal foetuses between 20 and 40 wk of gestation. Myocardial mechanical dyssynchrony and strain were assessed using offline quantification software (QLab Version 10.3, Philips Medical Systems, Andover, MA, USA). We compared the dyssynchrony measurements with TMAD and SLS in longitudinal and apical four-chamber views. Furthermore, we examined the segmental strain values of both ventricles with SLS and compared the differences between longitudinal and apical measurements. Dyssynchrony measurements with TMAD and SLS and strain measurements with SLS were feasible in all cases. In the apical view, the dyssynchrony measurements with TMAD were systematically greater than those achieved with SLS (p < 0.001). For the longitudinal view, no differences were observed between tools (p?=?0.153). The application of SLS provided similar results for dyssynchrony in both views (intra-class correlation coefficient [ICC]?=?0.281, p?=?0.623), but the strain measurements in the left and right ventricles differed significantly between views (ICC?=?–0.082, p?=?0.011, and ICC?=?–0.061, p?=?0.024, respectively). For TMAD, we found large differences in the dyssynchrony values between longitudinal and apical assessment (ICC?=?–0.060, p?=?0.03). Furthermore, TMAD exhibited reduced accuracy in the system's automatic tracking algorithm, limiting the data quality. The dyssynchrony assessment is affected less by the foetal position in SLS than in TMAD. The strain readings in SLS varied depending on the view in which they were assessed. The application of TMAD cannot be recommended for foetal STE.